Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

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weight		 Rot
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 DOI
155491018 174081 None 1 Human Functional pEC50 = 7.9 7.9 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Functional pEC50 = 7.9 7.9 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
10585 1078 None 1 Human Functional pEC50 = 7.9 7.9 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Functional pEC50 = 7.9 7.9 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Functional pEC50 = 7.9 7.9 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 174081 None 1 Human Functional pEC50 = 7.9 7.9 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Functional pEC50 = 7.9 7.9 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
10585 1078 None 1 Human Functional pEC50 = 7.9 7.9 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Functional pEC50 = 7.9 7.9 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Functional pEC50 = 7.9 7.9 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 174081 None 1 Human Functional pEC50 = 6.9 6.9 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Functional pEC50 = 6.9 6.9 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 174081 None 1 Human Functional pEC50 = 6.8 6.8 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Functional pEC50 = 6.8 6.8 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
44453327 95093 None 25 Human Functional pEC50 = 7.7 7.7 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL255408 95093 None 25 Human Functional pEC50 = 7.7 7.7 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
10585 1078 None 1 Human Functional pEC50 = 7.6 7.6 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Functional pEC50 = 7.6 7.6 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Functional pEC50 = 7.6 7.6 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1078 None 1 Human Functional pEC50 = 7.6 7.6 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Functional pEC50 = 7.6 7.6 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Functional pEC50 = 7.6 7.6 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 174081 None 1 Human Functional pEC50 = 7.5 7.5 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Functional pEC50 = 7.5 7.5 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 174081 None 1 Human Functional pEC50 = 7.5 7.5 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Functional pEC50 = 7.5 7.5 -2 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
69212799 77974 None 3 Human Functional pEC50 = 6.4 6.4 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL2096789 77974 None 3 Human Functional pEC50 = 6.4 6.4 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
508750 168533 None 1 Human Functional pEC50 = 7.4 7.4 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL435499 168533 None 1 Human Functional pEC50 = 7.4 7.4 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
10585 1078 None 1 Human Functional pEC50 = 7.3 7.3 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Functional pEC50 = 7.3 7.3 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Functional pEC50 = 7.3 7.3 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1078 None 1 Human Functional pEC50 = 7.3 7.3 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Functional pEC50 = 7.3 7.3 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Functional pEC50 = 7.3 7.3 1 2
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
44395055 64502 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL181432 64502 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
73351183 93232 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2448120 93232 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
70697571 77973 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2096788 77973 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
11735999 189348 None 0 Human Functional pED50 = 10.4 10.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 212 1 2 2 0.8 CC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL512607 189348 None 0 Human Functional pED50 = 10.4 10.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 212 1 2 2 0.8 CC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11322108 178565 None 0 Human Functional pED50 = 10.2 10.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 226 3 2 2 1.2 CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL467070 178565 None 0 Human Functional pED50 = 10.2 10.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 226 3 2 2 1.2 CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11254190 189350 None 0 Human Functional pED50 = 10.1 10.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 268 5 2 2 2.2 CC(C)CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL512615 189350 None 0 Human Functional pED50 = 10.1 10.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 268 5 2 2 2.2 CC(C)CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11651747 173767 None 0 Human Functional pED50 = 10.1 10.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 252 2 2 2 1.7 CC1(C(=O)N[C@H]2CCCCNC2=O)CCCCC1 10.1021/jm900133w
CHEMBL453720 173767 None 0 Human Functional pED50 = 10.1 10.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 252 2 2 2 1.7 CC1(C(=O)N[C@H]2CCCCNC2=O)CCCCC1 10.1021/jm900133w
11659300 178762 None 0 Human Functional pED50 = 10.1 10.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
CHEMBL468733 178762 None 0 Human Functional pED50 = 10.1 10.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
11151928 189485 None 0 Human Functional pED50 = 10.1 10.1 1 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL513863 189485 None 0 Human Functional pED50 = 10.1 10.1 1 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11173161 188805 None 0 Human Functional pED50 = 9.7 9.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 266 4 2 2 2.2 CC(C)=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL506023 188805 None 0 Human Functional pED50 = 9.7 9.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 266 4 2 2 2.2 CC(C)=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157844 189287 None 0 Human Functional pED50 = 9.4 9.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
CHEMBL512094 189287 None 0 Human Functional pED50 = 9.4 9.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
11218678 170351 None 0 Human Functional pED50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 240 4 2 2 1.6 CCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL444736 170351 None 0 Human Functional pED50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 240 4 2 2 1.6 CCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11543222 193505 None 3 Human Functional pED50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 2 2 2 1.4 O=C(N[C@H]1CCCCNC1=O)C1CCCCC1 10.1021/jm900133w
CHEMBL526704 193505 None 3 Human Functional pED50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 2 2 2 1.4 O=C(N[C@H]1CCCCNC1=O)C1CCCCC1 10.1021/jm900133w
11536008 178592 None 0 Human Functional pED50 = 9.1 9.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 236 2 2 2 1.3 O=C(N[C@H]1CCCCNC1=O)C1=CCCCC1 10.1021/jm900133w
CHEMBL467276 178592 None 0 Human Functional pED50 = 9.1 9.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 236 2 2 2 1.3 O=C(N[C@H]1CCCCNC1=O)C1=CCCCC1 10.1021/jm900133w
11551248 178658 None 0 Human Functional pED50 = 9.1 9.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 304 3 2 2 2.4 O=C(CC12CC3CC(CC(C3)C1)C2)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL467685 178658 None 0 Human Functional pED50 = 9.1 9.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 304 3 2 2 2.4 O=C(CC12CC3CC(CC(C3)C1)C2)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11390777 172614 None 0 Human Functional pED50 = 9 9.0 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 4 2 2 1.4 C=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL449215 172614 None 0 Human Functional pED50 = 9 9.0 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 4 2 2 1.4 C=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11198073 178477 None 0 Human Functional pED50 = 8 8.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 322 10 2 2 3.9 CCCCCCCCC/C=C(\C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466434 178477 None 0 Human Functional pED50 = 8 8.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 322 10 2 2 3.9 CCCCCCCCC/C=C(\C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11370332 63294 None 0 Human Functional pED50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 310 11 2 2 3.7 CCCCCCCCCCCC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL179312 63294 None 0 Human Functional pED50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 310 11 2 2 3.7 CCCCCCCCCCCC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157843 178475 None 0 Human Functional pED50 = 6.7 6.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466432 178475 None 0 Human Functional pED50 = 6.7 6.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157843 178475 None 0 Human Functional pED50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466432 178475 None 0 Human Functional pED50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11151929 178761 None 0 Human Functional pED50 = 8.4 8.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCC(C)(C)CC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL468732 178761 None 0 Human Functional pED50 = 8.4 8.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCC(C)(C)CC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11359715 178760 None 0 Human Functional pED50 = 8.4 8.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL468720 178760 None 0 Human Functional pED50 = 8.4 8.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@@H]1CCCCNC1=O 10.1021/jm900133w
11544064 178476 None 0 Human Functional pED50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 308 6 2 2 3.2 CCCCCC1CCC(C(=O)N[C@H]2CCCCNC2=O)CC1 10.1021/jm900133w
CHEMBL466433 178476 None 0 Human Functional pED50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 308 6 2 2 3.2 CCCCCC1CCC(C(=O)N[C@H]2CCCCNC2=O)CC1 10.1021/jm900133w
11609693 189210 None 0 Human Functional pED50 = 8.2 8.2 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 334 6 2 2 3.7 CCCCCC12CCC(C(=O)N[C@H]3CCCCNC3=O)(CC1)CC2 10.1021/jm900133w
CHEMBL511426 189210 None 0 Human Functional pED50 = 8.2 8.2 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 334 6 2 2 3.7 CCCCCC12CCC(C(=O)N[C@H]3CCCCNC3=O)(CC1)CC2 10.1021/jm900133w
11437477 188622 None 0 Human Functional pED50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 280 4 2 2 1.3 CC(CCl)(CCl)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL502976 188622 None 0 Human Functional pED50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 280 4 2 2 1.3 CC(CCl)(CCl)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44593562 187493 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187493 None 0 Human Functional pIC50 = 10 10.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
86642531 138301 None 0 Human Functional pIC50 = 9.9 9.9 10 2
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770912 138301 None 0 Human Functional pIC50 = 9.9 9.9 10 2
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
44425645 86080 None 0 Human Functional pIC50 = 9.8 9.8 7 2
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86080 None 0 Human Functional pIC50 = 9.8 9.8 7 2
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10240064 188426 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 188426 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593562 187493 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187493 None 0 Human Functional pIC50 = 9.7 9.7 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
44425652 168766 None 0 Human Functional pIC50 = 9.6 9.6 12 2
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168766 None 0 Human Functional pIC50 = 9.6 9.6 12 2
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
10289827 187974 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187974 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593563 193108 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193108 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
44425647 86099 None 0 Human Functional pIC50 = 9.5 9.5 5 2
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86099 None 0 Human Functional pIC50 = 9.5 9.5 5 2
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425292 85966 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230281 85966 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425292 85966 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230281 85966 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
10240064 188426 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 188426 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
46865775 8112 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091605 8112 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
24801689 97792 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97792 None 0 Human Functional pIC50 = 9.3 9.3 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
44425255 168882 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438304 168882 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425652 168766 None 0 Human Functional pIC50 = 9.2 9.2 12 2
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168766 None 0 Human Functional pIC50 = 9.2 9.2 12 2
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
59370257 138162 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 2 2 6 1.9 Cc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769444 138162 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 2 2 6 1.9 Cc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
10129192 188457 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL502793 188457 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
11598 672 None 9 Human Functional pIC50 = 9.2 9.2 812 2
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
23725177 672 None 9 Human Functional pIC50 = 9.2 9.2 812 2
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4442783 672 None 9 Human Functional pIC50 = 9.2 9.2 812 2
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
44425254 142258 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388487 142258 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 153527 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397996 153527 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425645 86080 None 0 Human Functional pIC50 = 9.2 9.2 7 2
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86080 None 0 Human Functional pIC50 = 9.2 9.2 7 2
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11597 673 None 5 Human Functional pIC50 = 9.1 9.1 11 2
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
23725180 673 None 5 Human Functional pIC50 = 9.1 9.1 11 2
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4781426 673 None 5 Human Functional pIC50 = 9.1 9.1 11 2
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
51039119 176215 None 33 Human Functional pIC50 = 9.1 9.1 -1 3
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176215 None 33 Human Functional pIC50 = 9.1 9.1 -1 3
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
44593564 187230 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187230 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
25022597 95337 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 95337 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
44453440 97686 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97686 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
183790 3740 None 11 Human Functional pIC50 = 9.0 9.0 -1 5
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3740 None 11 Human Functional pIC50 = 9.0 9.0 -1 5
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3740 None 11 Human Functional pIC50 = 9.0 9.0 -1 5
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
183790 3740 None 11 Human Functional pIC50 = 9.0 9.0 -1 5
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3740 None 11 Human Functional pIC50 = 9.0 9.0 -1 5
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3740 None 11 Human Functional pIC50 = 9.0 9.0 -1 5
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
24801690 98039 None 25 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 98039 None 25 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
57402219 71006 None 0 Human Functional pIC50 = 9 9.0 52 2
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71006 None 0 Human Functional pIC50 = 9 9.0 52 2
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
24801690 98039 None 25 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98039 None 25 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44593564 187230 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187230 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
44573649 187233 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492569 187233 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
44593562 187493 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187493 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
10175425 193531 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526752 193531 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
127025088 138261 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 420 3 2 6 1.8 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C4CC4)cs3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770530 138261 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 420 3 2 6 1.8 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C4CC4)cs3)CC2)C1 10.1039/C5MD00362H
127025086 138181 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 442 4 2 6 2.3 CC(C)c1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769610 138181 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 442 4 2 6 2.3 CC(C)c1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
46865774 8111 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091604 8111 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
86642531 138301 None 0 Rat Functional pIC50 = 8.9 8.9 -10 2
Antagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium fluxAntagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium flux
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770912 138301 None 0 Rat Functional pIC50 = 8.9 8.9 -10 2
Antagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium fluxAntagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium flux
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
10007642 19107 None 0 Human Functional pIC50 = 8.9 8.9 2 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19107 None 0 Human Functional pIC50 = 8.9 8.9 2 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
10218403 187908 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL496630 187908 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
46886055 8042 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albumin
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090893 8042 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albumin
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
127025093 138212 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 4 2 6 1.7 CCc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769984 138212 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 4 2 6 1.7 CCc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
46830335 8213 None 8 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8213 None 8 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
11365166 74542 None 1 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74542 None 1 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
52941377 19327 None 0 Human Functional pIC50 = 8.7 8.7 7 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19327 None 0 Human Functional pIC50 = 8.7 8.7 7 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
16216716 153527 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397996 153527 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425292 85966 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230281 85966 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 153527 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397996 153527 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11353855 74547 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74547 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44425652 168766 None 0 Human Functional pIC50 = 8.7 8.7 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL437359 168766 None 0 Human Functional pIC50 = 8.7 8.7 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425652 168766 None 0 Human Functional pIC50 = 8.7 8.7 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL437359 168766 None 0 Human Functional pIC50 = 8.7 8.7 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
57335017 70336 None 0 Human Functional pIC50 = 8 8.0 1380 2
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70336 None 0 Human Functional pIC50 = 8 8.0 1380 2
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
70691785 73725 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018391 73725 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
46830336 7848 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7848 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
54754967 77828 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL2092884 77828 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
10239991 188445 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 188445 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
57391766 71015 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951776 71015 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
10187492 147788 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147788 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
25256791 187689 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
CHEMBL495202 187689 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
11502371 153126 None 3 Human Functional pIC50 = 7 7.0 22 2
Antagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 153126 None 3 Human Functional pIC50 = 7 7.0 22 2
Antagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
11502371 153126 None 3 Human Functional pIC50 = 7 7.0 22 2
Antagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 153126 None 3 Human Functional pIC50 = 7 7.0 22 2
Antagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
10154434 58787 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 342 4 2 5 3.2 CC(C)Oc1cccc(NC(=O)NC(=O)c2ccc3c(c2)OCO3)c1 10.1021/jm1012903
CHEMBL1687955 58787 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 342 4 2 5 3.2 CC(C)Oc1cccc(NC(=O)NC(=O)c2ccc3c(c2)OCO3)c1 10.1021/jm1012903
44413167 79717 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211560 79717 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
9967878 85077 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 342 4 2 3 3.9 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1F 10.1016/j.bmc.2006.09.052
CHEMBL224510 85077 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 342 4 2 3 3.9 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1F 10.1016/j.bmc.2006.09.052
44421867 85155 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1cc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cs1 10.1016/j.bmc.2006.09.052
CHEMBL225166 85155 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1cc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cs1 10.1016/j.bmc.2006.09.052
44421889 85217 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCCC(Oc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225582 85217 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCCC(Oc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098519 85228 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 336 5 2 4 3.6 COc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225637 85228 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 336 5 2 4 3.6 COc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098523 142287 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 320 4 2 3 3.9 Cc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL388516 142287 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 320 4 2 3 3.9 Cc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421913 161882 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 334 4 2 3 3.4 O=C(Nc1ccc2[nH]ncc2c1)C1CCCN(Cc2ccccc2)C1 10.1016/j.bmc.2006.09.052
CHEMBL415061 161882 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 334 4 2 3 3.4 O=C(Nc1ccc2[nH]ncc2c1)C1CCCN(Cc2ccccc2)C1 10.1016/j.bmc.2006.09.052
21098488 166265 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL426925 166265 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098490 166323 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL427245 166323 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421917 166325 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL427254 166325 None 0 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
9840006 142024 None 5 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL387625 142024 None 5 Human Functional pIC50 = 6 6.0 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
9956238 60196 None 1 Rat Functional pIC50 = 5 5.0 -79 4
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60196 None 1 Rat Functional pIC50 = 5 5.0 -79 4
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60196 None 1 Rat Functional pIC50 = 5 5.0 -79 4
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
44453002 155371 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 7 2 3 3.9 O=C(CCNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL403424 155371 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 7 2 3 3.9 O=C(CCNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44421860 85046 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 295 4 3 3 3.0 c1c[nH]c(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224166 85046 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 295 4 3 3 3.0 c1c[nH]c(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
9900683 141910 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 292 4 2 3 3.2 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL386937 141910 None 0 Human Functional pIC50 = 5 5.0 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 292 4 2 3 3.2 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
10065796 142065 None 4 Human Functional pIC50 = 5 5.0 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 339 4 1 3 4.2 Fc1cccc(F)c1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL387954 142065 None 4 Human Functional pIC50 = 5 5.0 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 339 4 1 3 4.2 Fc1cccc(F)c1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
54585109 62571 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782579 62571 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
44453234 97469 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270182 97469 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
22143196 183985 None 0 Human Functional pIC50 = 7.0 7.0 -3 2
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183985 None 0 Human Functional pIC50 = 7.0 7.0 -3 2
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143196 183985 None 0 Human Functional pIC50 = 7.0 7.0 -3 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183985 None 0 Human Functional pIC50 = 7.0 7.0 -3 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44416138 138872 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138872 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46927117 65426 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829619 65426 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
44453405 95434 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
CHEMBL257062 95434 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
44453407 95435 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257063 95435 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
56675205 65793 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834788 65793 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
56671793 65794 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834789 65794 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56671795 65797 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834792 65797 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
46884856 8342 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092921 8342 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
44583280 172447 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 172447 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
46885159 8373 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1093153 8373 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
46885160 8374 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093154 8374 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
9974356 137589 None 4 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL375556 137589 None 4 Human Functional pIC50 = 5.0 5.0 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
57396726 68953 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 562 8 3 5 4.0 CS(=O)(=O)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
CHEMBL1922817 68953 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 562 8 3 5 4.0 CS(=O)(=O)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
44439163 90292 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238518 90292 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
183790 3740 None 11 Human Functional pIC50 = 7.9 7.9 -1 5
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
783 3740 None 11 Human Functional pIC50 = 7.9 7.9 -1 5
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
CHEMBL1178786 3740 None 11 Human Functional pIC50 = 7.9 7.9 -1 5
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
11283842 73736 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018402 73736 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11353855 74547 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74547 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56643545 68958 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68958 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
52943756 19288 None 0 Human Functional pIC50 = 7.9 7.9 23 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19288 None 0 Human Functional pIC50 = 7.9 7.9 23 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44453368 97765 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL271725 97765 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
56683116 65804 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834799 65804 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
46884898 7715 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7715 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
44453409 95437 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 95437 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
22143146 183904 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183904 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
10218843 172784 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451340 172784 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425641 86064 None 0 Human Functional pIC50 = 7.9 7.9 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230832 86064 None 0 Human Functional pIC50 = 7.9 7.9 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
10007642 19107 None 0 Mouse Functional pIC50 = 7.9 7.9 -2 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19107 None 0 Mouse Functional pIC50 = 7.9 7.9 -2 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
46885028 8420 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1093470 8420 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
24801523 97853 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97853 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
57656833 75227 None 0 Mouse Functional pIC50 = 5.9 5.9 -257 4
Antagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75227 None 0 Mouse Functional pIC50 = 5.9 5.9 -257 4
Antagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
122181148 121834 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 478 6 1 3 5.2 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589843 121834 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 478 6 1 3 5.2 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
9956238 60196 None 1 Mouse Functional pIC50 = 4.9 4.9 -95 4
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60196 None 1 Mouse Functional pIC50 = 4.9 4.9 -95 4
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60196 None 1 Mouse Functional pIC50 = 4.9 4.9 -95 4
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
508742 95574 None 1 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257702 95574 None 1 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
145963552 161346 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 489 6 1 5 4.1 CC(=O)N1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4125866 161346 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 489 6 1 5 4.1 CC(=O)N1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
122181146 121832 None 0 Human Functional pIC50 = 5.9 5.9 14 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589841 121832 None 0 Human Functional pIC50 = 5.9 5.9 14 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
44447435 94694 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252815 94694 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447435 94694 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252815 94694 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145962429 161567 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 446 6 1 4 5.4 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCCCC1 10.1016/j.bmc.2018.05.027
CHEMBL4128975 161567 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 446 6 1 4 5.4 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCCCC1 10.1016/j.bmc.2018.05.027
44453538 97928 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272543 97928 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
46240482 83575 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204259 83575 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
22143294 193424 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 193424 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44580590 193569 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 193569 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
70683350 73724 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018390 73724 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
44425641 86064 None 0 Human Functional pIC50 = 7.9 7.9 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230832 86064 None 0 Human Functional pIC50 = 7.9 7.9 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425288 86013 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230507 86013 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425304 143365 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL389773 143365 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
69035677 77647 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088389 77647 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
44425288 86013 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230507 86013 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425304 143365 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL389773 143365 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44571218 183876 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183876 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57344310 68934 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922794 68934 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57343820 68952 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922816 68952 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.113
24801525 97607 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97607 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
49763686 65422 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829615 65422 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
57396724 68945 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 485 7 2 3 4.1 NC(=O)C(NC1CCC(c2ccccc2)C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922805 68945 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 485 7 2 3 4.1 NC(=O)C(NC1CCC(c2ccccc2)C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57396725 68947 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 498 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)C2CC2c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922808 68947 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 498 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)C2CC2c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563039 192043 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 482 5 1 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL520228 192043 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 482 5 1 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11179439 73734 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018400 73734 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46947816 65431 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829624 65431 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
44563113 174581 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 515 5 3 4 5.4 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL455682 174581 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 515 5 3 4 5.4 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
508877 95059 None 1 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL255209 95059 None 1 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
54756045 65786 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834781 65786 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56678507 65798 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834793 65798 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44447429 94641 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252412 94641 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
50925394 19326 None 0 Mouse Functional pIC50 = 7.9 7.9 -2 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19326 None 0 Mouse Functional pIC50 = 7.9 7.9 -2 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
44447429 94641 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252412 94641 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425286 153245 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397750 153245 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425286 153245 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397750 153245 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
57344299 68954 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922818 68954 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
56669631 65807 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
CHEMBL1834851 65807 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
132572938 156787 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4070869 156787 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
44439158 146825 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
CHEMBL392493 146825 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
10272003 58877 None 1 Mouse Functional pIC50 = 5.9 5.9 -2 3
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58877 None 1 Mouse Functional pIC50 = 5.9 5.9 -2 3
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
57403700 68943 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.0 NC(=O)C(NC1Cc2ccccc2C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922803 68943 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.0 NC(=O)C(NC1Cc2ccccc2C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10427217 84995 None 4 Human Functional pIC50 = 4.9 4.9 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL223815 84995 None 4 Human Functional pIC50 = 4.9 4.9 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
10041590 142109 None 4 Human Functional pIC50 = 4.9 4.9 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL388285 142109 None 4 Human Functional pIC50 = 4.9 4.9 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
54584164 62566 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782574 62566 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44595711 137319 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium fluxAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium flux
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137319 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium fluxAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium flux
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
49763568 65413 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829605 65413 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
11752457 74537 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
CHEMBL2029417 74537 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
54755081 65775 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834719 65775 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56671794 65795 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834790 65795 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425634 142016 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL387587 142016 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44442599 93647 None 0 Human Functional pIC50 = 6.8 6.8 31 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93647 None 0 Human Functional pIC50 = 6.8 6.8 31 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
10291634 58875 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(Cl)c(Cl)c1 10.1021/jm1012903
CHEMBL1688879 58875 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(Cl)c(Cl)c1 10.1021/jm1012903
10154979 58876 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.4 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(C(F)(F)F)c1 10.1021/jm1012903
CHEMBL1688880 58876 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.4 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(C(F)(F)F)c1 10.1021/jm1012903
10064487 85015 None 4 Human Functional pIC50 = 4.8 4.8 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL223907 85015 None 4 Human Functional pIC50 = 4.8 4.8 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
11585168 90686 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239143 90686 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57402219 71006 None 0 Mouse Functional pIC50 = 6.8 6.8 -52 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71006 None 0 Mouse Functional pIC50 = 6.8 6.8 -52 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
145961260 161429 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 476 7 1 5 5.0 COC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127096 161429 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 476 7 1 5 5.0 COC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
52941377 19327 None 0 Mouse Functional pIC50 = 6.8 6.8 -7 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19327 None 0 Mouse Functional pIC50 = 6.8 6.8 -7 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
57394970 68941 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 465 7 2 3 4.0 CC(C)C1CCC(NC(C(N)=O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922800 68941 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 465 7 2 3 4.0 CC(C)C1CCC(NC(C(N)=O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2011.09.113
44583282 172693 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172693 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
53389660 171481 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 171481 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
53389845 172959 None 0 Human Functional pIC50 = 7.8 7.8 45 2
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172959 None 0 Human Functional pIC50 = 7.8 7.8 45 2
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
57344303 68929 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922789 68929 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44353447 3773 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
785 3773 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
CHEMBL337246 3773 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
44425634 142016 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL387587 142016 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11192346 2022 None 57 Mouse Functional pIC50 = 7.8 7.8 -4 3
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Mouse Functional pIC50 = 7.8 7.8 -4 3
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Mouse Functional pIC50 = 7.8 7.8 -4 3
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
44583281 188233 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 188233 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
49763575 65443 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829637 65443 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
24801522 161135 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 161135 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
46884855 8301 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092656 8301 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
122181235 121848 None 0 Human Functional pIC50 = 5.8 5.8 5 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589949 121848 None 0 Human Functional pIC50 = 5.8 5.8 5 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
9923015 58874 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 318 2 2 4 3.0 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(Cl)c1 10.1021/jm1012903
CHEMBL1688878 58874 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 318 2 2 4 3.0 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(Cl)c1 10.1021/jm1012903
11582651 75201 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036754 75201 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
145961759 161528 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 566 6 1 5 7.1 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(CC1)SCc1ccccc12 10.1016/j.bmc.2018.05.027
CHEMBL4128487 161528 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 566 6 1 5 7.1 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(CC1)SCc1ccccc12 10.1016/j.bmc.2018.05.027
57656921 75211 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036764 75211 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
122181152 121704 None 0 Human Functional pIC50 = 6.8 6.8 25 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3588870 121704 None 0 Human Functional pIC50 = 6.8 6.8 25 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
46241610 83568 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204252 83568 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
122181238 121851 None 0 Human Functional pIC50 = 7.8 7.8 194 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589952 121851 None 0 Human Functional pIC50 = 7.8 7.8 194 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
10304021 73718 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018384 73718 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
11504634 186034 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 4.6 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487070 186034 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 4.6 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
56678508 65799 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834794 65799 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44570718 183831 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480621 183831 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44580590 193569 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 193569 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
46944853 65428 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829621 65428 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
49763574 65442 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829636 65442 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755083 65742 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834636 65742 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
46885029 8247 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1092343 8247 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
10315045 143573 None 5 Human Functional pIC50 = 4.8 4.8 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL389926 143573 None 5 Human Functional pIC50 = 4.8 4.8 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
122181153 121838 None 0 Human Functional pIC50 = 6.8 6.8 20 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589847 121838 None 0 Human Functional pIC50 = 6.8 6.8 20 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
44416274 158552 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL409162 158552 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
10346048 78232 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL210606 78232 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
145962546 161408 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 6 3.8 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126779 161408 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 6 3.8 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
11553070 75198 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036751 75198 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10346048 78232 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL210606 78232 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
11563451 151916 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL396621 151916 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
24801690 98039 None 25 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 98039 None 25 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
70689914 74550 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74550 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
24801690 98039 None 25 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98039 None 25 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44453366 158302 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL408908 158302 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
46885027 8419 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8419 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
53322810 58470 None 0 Human Functional pIC50 = 7.7 7.7 2 2
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683075 58470 None 0 Human Functional pIC50 = 7.7 7.7 2 2
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54585107 62559 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62559 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54580188 62565 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782573 62565 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
53325639 58468 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683073 58468 None 0 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
122181147 121833 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 464 6 1 3 4.8 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589842 121833 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 464 6 1 3 4.8 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
11670910 88620 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL235657 88620 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
145961961 161494 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.0 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(C(F)(F)F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128015 161494 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.0 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(C(F)(F)F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
57656640 75209 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
CHEMBL2036762 75209 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
44439155 91972 None 0 Human Functional pIC50 = 6.7 6.7 -3 2
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241497 91972 None 0 Human Functional pIC50 = 6.7 6.7 -3 2
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46885269 7901 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CCN(C(=O)c2ccccc2)CC1)N1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1090148 7901 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CCN(C(=O)c2ccccc2)CC1)N1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2010.02.072
56643545 68958 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68958 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57398494 68956 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 527 8 3 4 4.7 CN(C)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
CHEMBL1922820 68956 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 527 8 3 4 4.7 CN(C)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
22143104 188056 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497780 188056 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
22143294 193424 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 193424 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44571257 191092 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL518772 191092 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11192346 2022 None 57 Human Functional pIC50 = 7.7 7.7 1 3
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Human Functional pIC50 = 7.7 7.7 1 3
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Human Functional pIC50 = 7.7 7.7 1 3
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
56661444 65773 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834717 65773 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44425637 85985 None 0 Human Functional pIC50 = 7.7 7.7 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230405 85985 None 0 Human Functional pIC50 = 7.7 7.7 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425637 85985 None 0 Human Functional pIC50 = 7.7 7.7 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230405 85985 None 0 Human Functional pIC50 = 7.7 7.7 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425629 86024 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230616 86024 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44442593 147198 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 147198 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
57344218 68946 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922806 68946 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563038 186037 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 1 5 5.0 CCOC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487074 186037 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 1 5 5.0 CCOC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
21098512 85087 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224594 85087 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098530 143557 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL389915 143557 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 351 5 2 5 3.5 O=[N+]([O-])c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44447426 94607 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252208 94607 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145961667 161352 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 461 6 1 5 4.2 CN1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4126007 161352 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 461 6 1 5 4.2 CN1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
44447426 94607 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252208 94607 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 8 1 2 7.0 C=CCC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145963369 161384 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 522 7 1 4 6.8 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC(c2ccccc2)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4126360 161384 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 522 7 1 4 6.8 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC(c2ccccc2)CC1 10.1016/j.bmc.2018.05.027
11548199 89920 None 0 Human Functional pIC50 = 8.7 8.7 707 2
Antagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium fluxAntagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium flux
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89920 None 0 Human Functional pIC50 = 8.7 8.7 707 2
Antagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium fluxAntagonist activity at CCR2 expressed in THP1 cells assessed as MCP1-induced calcium flux
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
22143255 187856 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187856 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143155 188060 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 188060 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44593555 188782 None 0 Human Functional pIC50 = 8.7 8.7 2 2
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188782 None 0 Human Functional pIC50 = 8.7 8.7 2 2
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44570714 189792 None 0 Human Functional pIC50 = 8.7 8.7 9 2
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL516224 189792 None 0 Human Functional pIC50 = 8.7 8.7 9 2
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
9850318 95243 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 95243 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
10392978 167457 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL429849 167457 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxisAntagonist activity at CCR2 receptor in human monocytes assessed as inhibition of MCP1-mediated chemotaxis
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
54754968 65740 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834634 65740 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425647 86099 None 0 Human Functional pIC50 = 8.7 8.7 5 2
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86099 None 0 Human Functional pIC50 = 8.7 8.7 5 2
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44423283 85305 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 85305 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44583283 188284 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500175 188284 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
127026243 138267 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 456 3 2 6 2.5 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770591 138267 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 456 3 2 6 2.5 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
53321616 58458 None 0 Human Functional pIC50 = 8.6 8.6 5 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683063 58458 None 0 Human Functional pIC50 = 8.6 8.6 5 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11433008 77635 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088378 77635 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
10289827 187974 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187974 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
25110716 155204 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxisAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxis
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL402532 155204 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxisAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced monocyte chemotaxis
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
53318853 58454 None 0 Human Functional pIC50 = 8.6 8.6 27 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683059 58454 None 0 Human Functional pIC50 = 8.6 8.6 27 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
11597 673 None 5 Human Functional pIC50 = 8.6 8.6 11 2
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
23725180 673 None 5 Human Functional pIC50 = 8.6 8.6 11 2
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4781426 673 None 5 Human Functional pIC50 = 8.6 8.6 11 2
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
11387511 74539 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029419 74539 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44453441 97687 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271289 97687 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
46885213 8458 None 0 Human Functional pIC50 = 8.6 8.6 52 3
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8458 None 0 Human Functional pIC50 = 8.6 8.6 52 3
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
57391767 71017 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951779 71017 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
127029034 138213 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 440 3 2 6 1.9 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(F)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770008 138213 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 440 3 2 6 1.9 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(C)(C)C)c(F)s3)CC2)C1 10.1039/C5MD00362H
11192346 2022 None 57 Rat Functional pIC50 = 8.6 8.6 -1 3
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Rat Functional pIC50 = 8.6 8.6 -1 3
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Rat Functional pIC50 = 8.6 8.6 -1 3
Antagonist activity at rat CCR2Antagonist activity at rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
10300284 73730 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018396 73730 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57396998 71012 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951773 71012 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
54755919 65757 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834651 65757 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
54755801 65758 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834652 65758 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
56659295 65808 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834852 65808 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425629 86024 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230616 86024 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
9956238 60196 None 1 Human Functional pIC50 = 6.7 6.7 3 4
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60196 None 1 Human Functional pIC50 = 6.7 6.7 3 4
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60196 None 1 Human Functional pIC50 = 6.7 6.7 3 4
Antagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human PBMC cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
57656833 75227 None 0 Rat Functional pIC50 = 6.7 6.7 -42 4
Antagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75227 None 0 Rat Functional pIC50 = 6.7 6.7 -42 4
Antagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at rat CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44421923 85080 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224535 85080 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
9857714 85129 None 2 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224885 85129 None 2 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421855 85112 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 2 4 3.0 c1cncc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224746 85112 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 2 4 3.0 c1cncc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
11723420 136549 None 5 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL373759 136549 None 5 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
57656887 75210 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036763 75210 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44447427 154845 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL400516 154845 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447427 154845 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL400516 154845 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 538 7 1 2 7.1 CC(C)C(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
11570431 91980 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241502 91980 None 0 Human Functional pIC50 = 6.7 6.7 -2 2
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
22143346 172649 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172649 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
10175423 188444 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502515 188444 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
10312346 188460 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 188460 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
10152864 187872 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187872 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
49763931 65424 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829617 65424 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
44453330 95500 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257316 95500 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
44453300 97434 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL270005 97434 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44416274 158552 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL409162 158552 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
24801523 97853 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97853 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
10458152 77799 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL209267 77799 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
10458152 77799 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL209267 77799 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
49764446 65438 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829631 65438 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
44453474 97869 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272284 97869 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
56659196 65801 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834796 65801 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
22143258 183877 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183877 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
57656942 75037 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2035000 75037 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57403699 68935 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cnccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922795 68935 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cnccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453004 95262 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 6 2 3 3.9 CC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL256256 95262 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 6 2 3 3.9 CC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10471319 84801 None 5 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 321 4 1 3 4.1 Fc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL223336 84801 None 5 Human Functional pIC50 = 4.7 4.7 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 321 4 1 3 4.1 Fc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
44439169 90772 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239170 90772 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44447446 154877 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL400724 154877 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44447424 94606 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252206 94606 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447446 154877 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL400724 154877 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11306757 73735 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018401 73735 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11489078 73803 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018530 73803 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44570781 192563 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 192563 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
46830335 8213 None 8 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8213 None 8 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
46842383 8343 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8343 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
70689915 74551 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74551 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
44453472 155536 None 1 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155536 None 1 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
54586021 62541 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62541 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
57396723 68944 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.5 NC(=O)C(NC1CCc2ccccc21)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922804 68944 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.5 NC(=O)C(NC1CCc2ccccc21)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10360623 85204 None 5 Human Functional pIC50 = 4.6 4.6 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 351 4 1 3 5.0 Clc1ccc(CN2CCCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL225492 85204 None 5 Human Functional pIC50 = 4.6 4.6 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 351 4 1 3 5.0 Clc1ccc(CN2CCCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
44447424 94606 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252206 94606 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 CC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44583280 172447 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 172447 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
10281316 73720 None 0 Human Functional pIC50 = 7.6 7.6 -2 3
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73720 None 0 Human Functional pIC50 = 7.6 7.6 -2 3
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
44453327 95093 None 25 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL255408 95093 None 25 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10162782 73704 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018370 73704 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44442590 93770 None 0 Human Functional pIC50 = 6.6 6.6 169 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93770 None 0 Human Functional pIC50 = 6.6 6.6 169 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
49763804 65423 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829616 65423 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
11510932 75200 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036753 75200 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
145962732 161355 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 554 8 0 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Oc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126032 161355 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 554 8 0 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Oc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44580591 187857 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187857 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
49763682 65419 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829612 65419 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44447432 154846 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL400517 154846 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44447432 154846 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL400517 154846 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CCC(CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
50991056 62564 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62564 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57394966 68925 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 495 6 2 2 6.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CNC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922785 68925 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 495 6 2 2 6.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CNC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
145953092 161336 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3cnc(Nc4ccc(Cl)c(Cl)c4)cc3C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4125768 161336 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3cnc(Nc4ccc(Cl)c(Cl)c4)cc3C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
22143309 187939 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187939 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
10111333 175465 None 0 Human Functional pIC50 = 7.6 7.6 19 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175465 None 0 Human Functional pIC50 = 7.6 7.6 19 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10142792 93739 None 0 Human Functional pIC50 = 6.6 6.6 26 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93739 None 0 Human Functional pIC50 = 6.6 6.6 26 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
57656869 75219 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036774 75219 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
52943756 19288 None 0 Mouse Functional pIC50 = 6.6 6.6 -23 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19288 None 0 Mouse Functional pIC50 = 6.6 6.6 -23 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
49764196 65440 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829633 65440 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44570717 183830 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL480620 183830 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
56676474 65810 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834854 65810 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
183790 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
783 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
CHEMBL1178786 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/s0960-894x(00)00347-4
44425309 142355 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388867 142355 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
183790 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
783 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
CHEMBL1178786 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Inhibition of chemotactic protein to CCR2bInhibition of chemotactic protein to CCR2b
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm010468s
183790 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Functional pIC50 = 7.6 7.6 -1 5
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
22143334 187806 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187806 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
57344297 68951 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922815 68951 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 10.1016/j.bmcl.2011.09.113
11711078 75218 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036773 75218 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46240584 83578 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
CHEMBL2204262 83578 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
46944854 65427 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829620 65427 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
54756156 65783 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834779 65783 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44447431 94669 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252611 94669 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425642 142344 None 0 Human Functional pIC50 = 7.6 7.6 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL388675 142344 None 0 Human Functional pIC50 = 7.6 7.6 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44447431 94669 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252611 94669 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425642 142344 None 0 Human Functional pIC50 = 7.6 7.6 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL388675 142344 None 0 Human Functional pIC50 = 7.6 7.6 12 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11678573 90637 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238936 90637 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57656713 75203 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036756 75203 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
44447433 94692 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252813 94692 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44447433 94692 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252813 94692 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
22143293 188025 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188025 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44447434 94693 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252814 94693 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44453535 155172 None 1 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402322 155172 None 1 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
44447434 94693 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL252814 94693 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
155521447 170582 None 0 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170582 None 0 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
11227168 74548 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74548 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
46884818 7869 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089881 7869 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
145963669 161557 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cc(Cl)cc(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128832 161557 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cc(Cl)cc(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44416157 80593 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80593 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
22143309 187939 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187939 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
22143112 188443 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 188443 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
57395219 71009 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
CHEMBL1951770 71009 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
11756884 19087 None 0 Human Functional pIC50 = 8.5 8.5 25 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19087 None 0 Human Functional pIC50 = 8.5 8.5 25 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
54754969 65738 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834632 65738 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
44425645 86080 None 0 Human Functional pIC50 = 8.5 8.5 7 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230933 86080 None 0 Human Functional pIC50 = 8.5 8.5 7 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44453442 97688 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271290 97688 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425645 86080 None 0 Human Functional pIC50 = 8.5 8.5 7 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230933 86080 None 0 Human Functional pIC50 = 8.5 8.5 7 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57395217 71007 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951768 71007 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
50992246 58469 None 2 Human Functional pIC50 = 8.5 8.5 -1 5
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58469 None 2 Human Functional pIC50 = 8.5 8.5 -1 5
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
50992246 58469 None 2 Human Functional pIC50 = 8.5 8.5 -1 5
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58469 None 2 Human Functional pIC50 = 8.5 8.5 -1 5
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44593561 12661 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12661 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12661 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
11192346 2022 None 57 Human Functional pIC50 = 8.5 8.5 1 3
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Human Functional pIC50 = 8.5 8.5 1 3
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Human Functional pIC50 = 8.5 8.5 1 3
Inhibition of CCR2-mediated calcium mobilizationInhibition of CCR2-mediated calcium mobilization
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
67011331 74543 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74543 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44425653 86227 None 0 Human Functional pIC50 = 8.5 8.5 4 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231246 86227 None 0 Human Functional pIC50 = 8.5 8.5 4 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425290 153529 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397997 153529 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11627639 94931 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assayAntagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assay
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL254355 94931 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assayAntagonist activity at CCR2 receptor expressed in THP1 cells assessed as MCP-1-induced calcium flux by chemotaxis assay
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44425653 86227 None 0 Human Functional pIC50 = 8.5 8.5 4 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231246 86227 None 0 Human Functional pIC50 = 8.5 8.5 4 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425290 153529 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397997 153529 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44453472 155536 None 1 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155536 None 1 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
24801689 97792 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97792 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
46830336 7848 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7848 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
11421712 74541 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74541 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10008367 2020 None 50 Human Functional pIC50 = 8.4 8.4 2 3
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2020 None 50 Human Functional pIC50 = 8.4 8.4 2 3
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2020 None 50 Human Functional pIC50 = 8.4 8.4 2 3
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2020 None 50 Human Functional pIC50 = 8.4 8.4 2 3
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
44425647 86099 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231039 86099 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57395218 71008 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951769 71008 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
11192346 2022 None 57 Human Functional pIC50 = 8.4 8.4 1 3
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Human Functional pIC50 = 8.4 8.4 1 3
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Human Functional pIC50 = 8.4 8.4 1 3
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
50992246 58469 None 2 Human Functional pIC50 = 8.4 8.4 -1 5
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58469 None 2 Human Functional pIC50 = 8.4 8.4 -1 5
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
508869 95438 None 1 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257066 95438 None 1 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425647 86099 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231039 86099 None 0 Human Functional pIC50 = 8.4 8.4 5 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425643 86040 None 0 Human Functional pIC50 = 8.4 8.4 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230722 86040 None 0 Human Functional pIC50 = 8.4 8.4 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
46241717 83565 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204249 83565 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46208367 83579 None 13 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83579 None 13 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
24801522 161135 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 161135 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
56657929 65790 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834785 65790 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
46842383 8343 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8343 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
44425308 153704 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL398150 153704 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
10111333 175465 None 0 Human Functional pIC50 = 7.5 7.5 19 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175465 None 0 Human Functional pIC50 = 7.5 7.5 19 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
44425308 153704 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL398150 153704 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
54585107 62559 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62559 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44353447 3773 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3773 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3773 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
137654404 158567 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C(=O)N(CC(C)C)CC(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)=C3)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4091736 158567 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C(=O)N(CC(C)C)CC(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)=C3)cc1 10.1016/j.ejmech.2017.04.046
44421922 144548 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL390736 144548 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
9836178 85075 None 2 Human Functional pIC50 = 4.5 4.5 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224500 85075 None 2 Human Functional pIC50 = 4.5 4.5 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 306 4 2 3 3.6 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
10245340 168935 None 5 Human Functional pIC50 = 4.5 4.5 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL438783 168935 None 5 Human Functional pIC50 = 4.5 4.5 - 1
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
67011331 74543 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74543 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57656657 75207 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036760 75207 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
56671792 65792 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834787 65792 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
162666730 182272 None 1 Human Functional pIC50 = 7.5 7.5 562 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Functional pIC50 = 7.5 7.5 562 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
122181149 121835 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 494 7 1 4 4.8 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589844 121835 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 494 7 1 4 4.8 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
11534473 90697 None 0 Human Functional pIC50 = 7.5 7.5 117 2
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
CHEMBL239144 90697 None 0 Human Functional pIC50 = 7.5 7.5 117 2
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
10117480 73714 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018380 73714 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
70688149 75222 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036777 75222 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44296219 101312 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 435 4 1 5 5.2 Cc1ccc2c(c1)C1(CCN(CCc3nc(-c4ccc(F)cc4)oc3C)CC1)OC(=O)N2 10.1016/s0960-894x(00)00347-4
CHEMBL296609 101312 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against C-C chemokine receptor type 2
ChEMBL 435 4 1 5 5.2 Cc1ccc2c(c1)C1(CCN(CCc3nc(-c4ccc(F)cc4)oc3C)CC1)OC(=O)N2 10.1016/s0960-894x(00)00347-4
44442598 154385 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 154385 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
71452241 83566 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204250 83566 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
10120067 73727 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018393 73727 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
70689914 74550 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74550 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
70689915 74551 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74551 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
162666730 182272 None 1 Human Functional pIC50 = 7.5 7.5 562 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Functional pIC50 = 7.5 7.5 562 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
56659197 65802 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834797 65802 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
22725647 173697 None 0 Human Functional pIC50 = 7.5 7.5 52 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173697 None 0 Human Functional pIC50 = 7.5 7.5 52 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155521447 170582 None 0 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170582 None 0 Human Functional pIC50 = 6.5 6.5 3 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
145954949 161642 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 2 6 3.9 CS(=O)(=O)NC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4130191 161642 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 2 6 3.9 CS(=O)(=O)NC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
10129343 173263 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 173263 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
56668309 65774 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834718 65774 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
54756038 65776 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834720 65776 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
49763571 65416 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829609 65416 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
46945254 65433 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829626 65433 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
57344305 68937 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922797 68937 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453373 97809 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271935 97809 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
54755079 65739 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
CHEMBL1834633 65739 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
3547 141371 None 71 Human Functional pIC50 = 4.5 4.5 -8 8
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
CHEMBL38380 141371 None 71 Human Functional pIC50 = 4.5 4.5 -8 8
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
CHEMBL541388 141371 None 71 Human Functional pIC50 = 4.5 4.5 -8 8
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.09.052
3547 141371 None 71 Human Functional pIC50 = 4.5 4.5 -8 8
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
CHEMBL38380 141371 None 71 Human Functional pIC50 = 4.5 4.5 -8 8
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
CHEMBL541388 141371 None 71 Human Functional pIC50 = 4.5 4.5 -8 8
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 291 2 1 4 1.2 O=S(=O)(c1cccc2cnccc12)N1CCCNCC1 10.1016/j.bmc.2006.10.028
122181236 121849 None 0 Human Functional pIC50 = 6.5 6.5 13 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589950 121849 None 0 Human Functional pIC50 = 6.5 6.5 13 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
11319072 74540 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029420 74540 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57344296 68949 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922813 68949 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2011.09.113
23630215 62542 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62542 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
44453134 98062 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL273195 98062 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
67220645 75228 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036783 75228 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44453298 155237 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 155237 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44442599 93647 None 0 Human Functional pIC50 = 7.4 7.4 31 2
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93647 None 0 Human Functional pIC50 = 7.4 7.4 31 2
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
11353843 74545 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74545 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56683121 65809 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834853 65809 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
10196988 169463 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL442929 169463 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
57401954 68957 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922822 68957 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57656854 75226 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036781 75226 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
22143255 187856 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187856 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
10323427 79758 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL211775 79758 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
145953765 161523 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 7 4.2 CN(C1CCN(CCCn2ccc3c(Nc4ccc(Cl)c(Cl)c4)nccc3c2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128372 161523 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 7 4.2 CN(C1CCN(CCCn2ccc3c(Nc4ccc(Cl)c(Cl)c4)nccc3c2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
44442587 93807 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93807 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10323427 79758 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL211775 79758 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2008.01.023
10129343 173263 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 173263 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
145962575 161466 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 567 9 1 6 4.7 CCS(=O)(=O)N(C)C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127580 161466 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 567 9 1 6 4.7 CCS(=O)(=O)N(C)C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
10268598 58873 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 334 2 3 5 2.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(O)c(Cl)c1 10.1021/jm1012903
CHEMBL1688877 58873 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 334 2 3 5 2.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(O)c(Cl)c1 10.1021/jm1012903
10436083 79875 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212306 79875 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
44415880 169337 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 169337 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46241010 83582 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204266 83582 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
56643545 68958 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 by chemotaxis functional assayAntagonist activity at CCR2 by chemotaxis functional assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68958 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 by chemotaxis functional assayAntagonist activity at CCR2 by chemotaxis functional assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10281316 73720 None 0 Mouse Functional pIC50 = 8.4 8.4 2 3
Antagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73720 None 0 Mouse Functional pIC50 = 8.4 8.4 2 3
Antagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in mouse monocytes assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
25154827 174582 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL455683 174582 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
56657930 65791 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
CHEMBL1834786 65791 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
44425643 86040 None 0 Human Functional pIC50 = 8.4 8.4 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230722 86040 None 0 Human Functional pIC50 = 8.4 8.4 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
10120907 73722 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018388 73722 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
11227168 74548 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74548 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
11527661 2019 None 30 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2019 None 30 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2019 None 30 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
11527661 2019 None 30 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9045 2019 None 30 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL1963131 2019 None 30 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
22143346 172649 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172649 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
11753466 77638 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088380 77638 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
51039119 176215 None 33 Human Functional pIC50 = 8.3 8.3 -1 3
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176215 None 33 Human Functional pIC50 = 8.3 8.3 -1 3
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulationAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
24801526 97614 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97614 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
11330837 74549 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029570 74549 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56671925 65747 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834640 65747 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
22725647 173697 None 0 Human Functional pIC50 = 7.4 7.4 52 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173697 None 0 Human Functional pIC50 = 7.4 7.4 52 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
54582215 62558 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782566 62558 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10436083 79875 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212306 79875 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
9858433 85076 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 324 4 2 3 3.8 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL224509 85076 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 324 4 2 3 3.8 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
127025091 138208 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 424 3 2 7 1.2 COc1sc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)nc1C 10.1039/C5MD00362H
CHEMBL3769934 138208 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 424 3 2 7 1.2 COc1sc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)nc1C 10.1039/C5MD00362H
22143305 183610 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183610 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44425306 142367 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL388949 142367 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44453592 160053 None 24 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL410829 160053 None 24 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
44453565 169005 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439252 169005 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
49764447 65420 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829613 65420 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
24801525 97607 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97607 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
11598084 75202 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036755 75202 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
57656641 75220 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036775 75220 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44425306 142367 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL388949 142367 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
57656749 75208 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036761 75208 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44413147 139711 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL379818 139711 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
44413147 139711 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
CHEMBL379818 139711 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2008.01.023
46241718 83569 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204253 83569 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
44453471 97868 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272283 97868 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44453562 155652 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404837 155652 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10312346 188460 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 188460 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
54581190 62560 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782568 62560 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
70696470 75216 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036769 75216 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
46241608 83567 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204251 83567 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
11756884 19087 None 0 Mouse Functional pIC50 = 6.4 6.4 -25 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19087 None 0 Mouse Functional pIC50 = 6.4 6.4 -25 2
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
508729 95533 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257510 95533 None 1 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
145963612 161437 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 448 6 1 5 4.2 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCOCC1 10.1016/j.bmc.2018.05.027
CHEMBL4127249 161437 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 448 6 1 5 4.2 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCOCC1 10.1016/j.bmc.2018.05.027
54582216 62563 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782571 62563 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54583186 62570 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782578 62570 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
122181151 121837 None 0 Human Functional pIC50 = 6.3 6.3 7 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589846 121837 None 0 Human Functional pIC50 = 6.3 6.3 7 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
54754722 65750 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834643 65750 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44453171 95735 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL258364 95735 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
57344221 68955 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922819 68955 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
145955877 161402 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 503 8 1 6 3.1 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126634 161402 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 503 8 1 6 3.1 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
22143334 187806 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187806 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
10209478 73719 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
CHEMBL2018385 73719 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
11591776 145484 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL391459 145484 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
10239991 188445 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 188445 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593555 188782 None 0 Human Functional pIC50 = 8.3 8.3 2 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188782 None 0 Human Functional pIC50 = 8.3 8.3 2 2
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44453408 95436 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257064 95436 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44573608 187549 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494540 187549 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
10167417 73723 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018389 73723 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
44453440 97686 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97686 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44425293 153462 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397948 153462 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
22143155 188060 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 188060 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
11330529 74538 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029418 74538 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
22143146 183904 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183904 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44453298 155237 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 155237 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
57396999 71016 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951777 71016 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
11192943 77622 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088212 77622 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
53322809 58455 None 0 Human Functional pIC50 = 8.2 8.2 13 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683060 58455 None 0 Human Functional pIC50 = 8.2 8.2 13 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
57391765 71013 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
CHEMBL1951774 71013 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
69035439 77646 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088388 77646 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
57656833 75227 None 0 Human Functional pIC50 = 8.2 8.2 4 4
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75227 None 0 Human Functional pIC50 = 8.2 8.2 4 4
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10323427 79758 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79758 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytesAntagonist activity against CCR2 assessed as inhibition of MCP1-induced calcium flux in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
57400160 68923 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 3 5.6 O=C(O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922783 68923 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 3 5.6 O=C(O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
54584109 62545 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62545 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
44421868 85156 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 296 4 2 4 3.2 c1coc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL225167 85156 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 296 4 2 4 3.2 c1coc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098480 144141 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1cccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL390389 144141 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1cccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
145962604 161525 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 541 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(C(C)(C)C)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128399 161525 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 541 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(C(C)(C)C)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
11180383 77621 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088211 77621 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
22143200 187763 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495718 187763 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
44442586 93809 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93809 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10164316 154790 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400196 154790 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
56667036 65425 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829618 65425 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
56677288 65441 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829634 65441 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
11409228 74532 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029412 74532 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
46842084 7913 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1090206 7913 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
57396722 68942 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 536 4 3 3 5.0 O=C1NC2(CCC(c3c[nH]c4ccccc34)CC2)NC1C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922801 68942 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 536 4 3 3 5.0 O=C1NC2(CCC(c3c[nH]c4ccccc34)CC2)NC1C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
11721085 166857 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL428559 166857 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44353447 3773 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
46927116 65435 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829628 65435 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
57656871 75225 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036780 75225 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
145962608 161531 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 486 8 1 7 2.4 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccccn3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128514 161531 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 486 8 1 7 2.4 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccccn3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
46241509 83560 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204244 83560 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
44423283 85305 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxisAntagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxis
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 85305 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxisAntagonist activity against human CCR2 receptor in human monocytes assessed as inhibition of chemotaxis
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44442587 93807 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93807 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
46944855 65432 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829625 65432 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
44416273 138939 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL378449 138939 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44416273 138939 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL378449 138939 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
57656938 75213 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036766 75213 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44442590 93770 None 0 Human Functional pIC50 = 7.2 7.2 169 2
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93770 None 0 Human Functional pIC50 = 7.2 7.2 169 2
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442593 147198 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 147198 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11647276 75205 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036758 75205 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
70681778 75215 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
CHEMBL2036768 75215 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
11690139 75223 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036778 75223 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
57656719 75214 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036767 75214 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
56643545 68958 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 by calcium mobilization assayAntagonist activity at CCR2 by calcium mobilization assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68958 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 by calcium mobilization assayAntagonist activity at CCR2 by calcium mobilization assay
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44580591 187857 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187857 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
44571218 183876 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183876 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
22143258 183877 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183877 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11584094 188930 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL508015 188930 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 494 6 2 4 4.3 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11613399 188943 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 5.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL508073 188943 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 5.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11527661 2019 None 30 Human Functional pIC50 = 8.2 8.2 - 1
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2019 None 30 Human Functional pIC50 = 8.2 8.2 - 1
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2019 None 30 Human Functional pIC50 = 8.2 8.2 - 1
Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assayInhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
11353843 74545 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74545 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44453329 155349 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL403281 155349 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
53325639 58468 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58468 None 0 Human Functional pIC50 = 8.2 8.2 1 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
54583111 62543 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782377 62543 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44583281 188233 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 188233 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
11421712 74541 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74541 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
50925394 19326 None 0 Human Functional pIC50 = 8.2 8.2 2 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19326 None 0 Human Functional pIC50 = 8.2 8.2 2 2
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
53324304 58462 None 0 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58462 None 0 Human Functional pIC50 = 8.2 8.2 3 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
46240484 83577 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204261 83577 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
57394969 68938 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 499 7 2 3 4.5 NC(=O)C(NC1CCC(c2ccccc2)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922798 68938 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 499 7 2 3 4.5 NC(=O)C(NC1CCC(c2ccccc2)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44421888 85191 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCC(Oc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225434 85191 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCC(Oc3ccc4[nH]ncc4c3)CC2)cc1 10.1016/j.bmc.2006.09.052
44421862 136378 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1csc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL373512 136378 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1csc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
145961982 161530 None 0 Human Functional pIC50 = 7.2 7.2 10 2
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128498 161530 None 0 Human Functional pIC50 = 7.2 7.2 10 2
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.3 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
122181237 121850 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 574 7 2 4 6.0 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1cc(O)ccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589951 121850 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 574 7 2 4 6.0 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1cc(O)ccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
46842232 7880 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1089965 7880 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
11567495 75197 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036750 75197 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
24801526 97614 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97614 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
145953762 161432 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4127135 161432 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 539 8 1 6 3.9 CN(C1CCN(CCCN2CCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
10240278 172895 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451597 172895 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
57344298 68950 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922814 68950 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453409 95437 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 95437 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
57656715 75204 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036757 75204 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57344315 68939 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 10.1016/j.bmcl.2011.09.113
CHEMBL1922799 68939 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 10.1016/j.bmcl.2011.09.113
44447436 154690 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL399717 154690 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447436 154690 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL399717 154690 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 512 9 1 2 6.8 C=CCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
46240785 83580 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204264 83580 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
23630215 62542 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62542 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
54754724 65752 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834645 65752 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54580190 62569 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782577 62569 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46842235 7834 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089629 7834 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
49764322 65439 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829632 65439 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
11365166 74542 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74542 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
135981707 65788 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834783 65788 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
44425654 86228 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231247 86228 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425654 86228 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL231247 86228 None 0 Human Functional pIC50 = 7.2 7.2 2 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
57344316 68932 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922792 68932 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
46240687 83583 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204267 83583 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44439166 90544 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238731 90544 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
122181144 121830 None 0 Human Functional pIC50 = 6.2 6.2 35 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589839 121830 None 0 Human Functional pIC50 = 6.2 6.2 35 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
10182382 93960 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248418 93960 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
22143293 188025 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188025 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44583282 172693 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172693 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
22143241 183248 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479642 183248 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
56643545 68958 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68958 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
11591595 186155 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 512 6 2 4 4.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487238 186155 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 512 6 2 4 4.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
54755560 65777 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834721 65777 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56661451 65796 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834791 65796 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
56683044 65800 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834795 65800 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56662695 65803 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834798 65803 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
10232019 73728 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
CHEMBL2018394 73728 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
57398750 71014 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951775 71014 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
127025092 138221 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 414 2 2 6 1.5 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770125 138221 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 414 2 2 6 1.5 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(Cl)s3)CC2)C1 10.1039/C5MD00362H
10152864 187872 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187872 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
57391768 71011 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
CHEMBL1951772 71011 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
25022597 95337 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 95337 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced calcium flux
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
44425633 86039 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230721 86039 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425633 86039 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230721 86039 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
50991056 62564 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62564 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10008367 2020 None 50 Mouse Functional pIC50 = 8.1 8.1 -2 3
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2020 None 50 Mouse Functional pIC50 = 8.1 8.1 -2 3
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2020 None 50 Mouse Functional pIC50 = 8.1 8.1 -2 3
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2020 None 50 Mouse Functional pIC50 = 8.1 8.1 -2 3
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
44425635 153530 None 0 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL398000 153530 None 0 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
46240585 83581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204265 83581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44353447 3773 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3773 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3773 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
10272003 58877 None 1 Human Functional pIC50 = 6.2 6.2 2 3
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58877 None 1 Human Functional pIC50 = 6.2 6.2 2 3
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
10272003 58877 None 1 Human Functional pIC50 = 6.2 6.2 2 3
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58877 None 1 Human Functional pIC50 = 6.2 6.2 2 3
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
21098469 142350 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccccc1CN1CCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL388742 142350 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccccc1CN1CCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
54585108 62561 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782569 62561 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54583187 62572 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782580 62572 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
46885214 7696 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1)N1CCN(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1088810 7696 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1)N1CCN(C(=O)c2ccccc2)CC1 10.1016/j.bmcl.2010.02.072
145960485 161549 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 546 6 1 4 7.0 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(C=Cc3ccccc32)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4128742 161549 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 546 6 1 4 7.0 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(C=Cc3ccccc32)CC1 10.1016/j.bmc.2018.05.027
44442586 93809 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93809 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
54583112 62544 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782378 62544 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46241826 83559 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204243 83559 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
145954490 161633 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 519 8 1 6 3.6 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4130047 161633 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 519 8 1 6 3.6 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)cc3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
70693849 73729 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
CHEMBL2018395 73729 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
44453507 168976 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439062 168976 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
54583185 62562 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782570 62562 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57393249 68959 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C\c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922824 68959 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C\c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
22143196 183985 None 0 Human Functional pIC50 = 7.1 7.1 -3 2
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183985 None 0 Human Functional pIC50 = 7.1 7.1 -3 2
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143196 183985 None 0 Human Functional pIC50 = 7.1 7.1 -3 2
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183985 None 0 Human Functional pIC50 = 7.1 7.1 -3 2
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57656825 75206 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036759 75206 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46842086 7977 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1090548 7977 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
122181145 121831 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589840 121831 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
44413411 77736 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
CHEMBL209002 77736 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
44413411 77736 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
CHEMBL209002 77736 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2008.01.023
44453534 97879 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL272331 97879 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
44413144 139217 None 0 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL378784 139217 None 0 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
44413144 139217 None 0 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL378784 139217 None 0 Human Functional pIC50 = 6.1 6.1 -1 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
145960924 161543 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 581 10 1 6 4.2 CN(C1CCN(CCCN2CCCc3c(ccnc3NCCc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128658 161543 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 581 10 1 6 4.2 CN(C1CCN(CCCN2CCCc3c(ccnc3NCCc3ccc(Cl)c(Cl)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
162658125 181094 None 0 Human Functional pIC50 = 7.1 7.1 100 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Functional pIC50 = 7.1 7.1 100 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
57335017 70336 None 0 Human Functional pIC50 = 8.1 8.1 1380 2
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70336 None 0 Human Functional pIC50 = 8.1 8.1 1380 2
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.1% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10142792 93739 None 0 Human Functional pIC50 = 8.1 8.1 26 2
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93739 None 0 Human Functional pIC50 = 8.1 8.1 26 2
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22143112 188443 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 188443 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
22143305 183610 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183610 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44570781 192563 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 192563 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPRAntagonist activity at CCR2 in human monocytes assessed as inhibition of MCP1-induced calcium influx by FLIPR
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
56664979 65741 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834635 65741 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44425635 153530 None 0 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL398000 153530 None 0 Human Functional pIC50 = 8.1 8.1 3 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11421840 77636 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088379 77636 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
11273379 74546 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74546 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44453365 97525 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL270435 97525 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
53322810 58470 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58470 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425630 86025 None 0 Human Functional pIC50 = 8.1 8.1 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230617 86025 None 0 Human Functional pIC50 = 8.1 8.1 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
9956238 60196 None 1 Human Functional pIC50 = 7.1 7.1 3 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60196 None 1 Human Functional pIC50 = 7.1 7.1 3 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60196 None 1 Human Functional pIC50 = 7.1 7.1 3 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
9956238 60196 None 1 Human Functional pIC50 = 7.1 7.1 3 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60196 None 1 Human Functional pIC50 = 7.1 7.1 3 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60196 None 1 Human Functional pIC50 = 7.1 7.1 3 4
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs trans-well migration assay
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
21098478 142638 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL389168 142638 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1cccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
21098468 144671 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL390837 144671 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
68616341 73731 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018397 73731 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57400161 68924 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 3 5.9 CN(C1CCC(c2c[nH]c3ccccc23)CC1)C(C(=O)O)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922784 68924 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 3 5.9 CN(C1CCC(c2c[nH]c3ccccc23)CC1)C(C(=O)O)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44442598 154385 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 154385 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
11843812 79902 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212423 79902 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
11606702 145752 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391662 145752 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57344307 68936 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922796 68936 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44413399 79527 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211404 79527 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
11843812 79902 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL212423 79902 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2008.01.023
44413399 79527 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211404 79527 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
10187492 147788 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147788 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ fluxAntagonist activity at CCR2 in THP1 cells assessed as inhibition of MCP1-induced Ca2+ flux
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
54754723 65751 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834644 65751 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57394967 68926 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 509 6 2 2 6.5 CC(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922786 68926 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 509 6 2 2 6.5 CC(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44413137 78890 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
CHEMBL211292 78890 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
162658125 181094 None 0 Human Functional pIC50 = 7.1 7.1 100 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Functional pIC50 = 7.1 7.1 100 3
Antagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting methodAntagonist activity at human CCR2 expressed in human U2OS cell membranes as inhibition of [35S]GTPgammaS binding pre-incubated for 30 mins before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
44425308 153704 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL398150 153704 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44413137 78890 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
CHEMBL211292 78890 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2008.01.023
155514261 169834 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169834 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
155514261 169834 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4439854 169834 None 0 Human Functional pIC50 = 5.1 5.1 -1 2
Antagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assayAntagonist activity at human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor assessed as reduction in CCL2-induced G-protein activation preincubated for 30 mins in presence of CCL2 followed by incubation of 90 mins by [35S]GTPgammaS binding assay
ChEMBL 493 4 1 3 5.2 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1)C1CC1 10.1021/acs.jmedchem.8b00605
11273379 74546 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74546 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
122181150 121836 None 0 Human Functional pIC50 = 7.1 7.1 125 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589845 121836 None 0 Human Functional pIC50 = 7.1 7.1 125 2
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
781 3394 None 80 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)Inhibitory activity against C-C chemokine receptor type 2 (antagonist activity)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10165625 73726 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018392 73726 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
46884898 7715 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7715 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
46885027 8419 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8419 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
53325460 58492 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58492 None 0 Human Functional pIC50 = 8.1 8.1 2 2
Antagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at human CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
56671923 65737 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834631 65737 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
44425630 86025 None 0 Human Functional pIC50 = 8.1 8.1 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL230617 86025 None 0 Human Functional pIC50 = 8.1 8.1 14 2
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
127025089 138303 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 398 2 2 6 1.0 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(F)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770951 138303 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 398 2 2 6 1.0 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ncc(F)s3)CC2)C1 10.1039/C5MD00362H
44453325 155539 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
CHEMBL404269 155539 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
57395216 71010 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951771 71010 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
44453372 155742 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL405633 155742 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
10281715 73721 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018387 73721 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
54582217 62568 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782576 62568 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
57344314 68928 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922788 68928 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57394968 68927 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 7 3 3 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)NC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922787 68927 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 7 3 3 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)NC2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2011.09.113
57391487 68933 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 540 7 3 4 4.6 NC(=O)C(NC1CCC(C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922793 68933 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 540 7 3 4 4.6 NC(=O)C(NC1CCC(C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
70692344 75196 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036749 75196 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
57398493 68948 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 473 6 4 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922811 68948 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 473 6 4 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563071 186693 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 4 4.0 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL488433 186693 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 525 6 2 4 4.0 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
11632418 75195 None 1 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 75195 None 1 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44415898 81119 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL215654 81119 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
44415898 81119 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
CHEMBL215654 81119 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2008.01.023
57344317 68930 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922790 68930 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57344318 68931 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922791 68931 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44453327 95093 None 25 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL255408 95093 None 25 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
57393497 69130 None 0 Human Functional pKd = 6 6.0 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924022 69130 None 0 Human Functional pKd = 6 6.0 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
15985912 83973 None 0 Human Functional pKd = 5 5.0 - 0
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape changeAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape change
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83973 None 0 Human Functional pKd = 5 5.0 - 0
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape changeAntagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-stimulated monocyte shape change
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
57400128 69123 None 0 Human Functional pKd = 5.9 5.9 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924015 69123 None 0 Human Functional pKd = 5.9 5.9 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57400125 69112 None 0 Human Functional pKd = 5.8 5.8 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 69112 None 0 Human Functional pKd = 5.8 5.8 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44180522 69132 None 0 Human Functional pKd = 6.6 6.6 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924024 69132 None 0 Human Functional pKd = 6.6 6.6 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393496 69129 None 0 Human Functional pKd = 5.6 5.6 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924021 69129 None 0 Human Functional pKd = 5.6 5.6 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57656833 75227 None 0 Human Functional pKd = 8.5 8.5 4 4
Antagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin sheddingAntagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin shedding
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75227 None 0 Human Functional pKd = 8.5 8.5 4 4
Antagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin sheddingAntagonist activity at human CCR2 in human peripheral whole blood assessed as inhibition of MCP1-induced L-selectin shedding
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
57393219 69120 None 0 Human Functional pKd = 5.5 5.5 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924012 69120 None 0 Human Functional pKd = 5.5 5.5 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57400127 69122 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924014 69122 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57393220 69124 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924016 69124 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57397001 69126 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924018 69126 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57400420 69127 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924019 69127 None 0 Human Functional pKd = 6.4 6.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57393495 69128 None 0 Human Functional pKd = 5.4 5.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924020 69128 None 0 Human Functional pKd = 5.4 5.4 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400129 69125 None 0 Human Functional pKd = 6.3 6.3 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924017 69125 None 0 Human Functional pKd = 6.3 6.3 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57395221 69131 None 0 Human Functional pKd = 6.3 6.3 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924023 69131 None 0 Human Functional pKd = 6.3 6.3 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57398458 69121 None 0 Human Functional pKd = 6.2 6.2 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924013 69121 None 0 Human Functional pKd = 6.2 6.2 - 0
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of MCP-1 induced monocyte shape change pretreated for 15 mins before MCP-1 challenge measured after 5 mins by flow cytometry
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
16124598 10727 None 0 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171008 10727 None 0 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798435 10701 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170828 10701 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
49798434 10700 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 490 6 2 5 5.5 O=C(O)c1c(F)cccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170827 10700 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 490 6 2 5 5.5 O=C(O)c1c(F)cccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798461 10691 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170725 10691 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
17756652 10728 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 473 6 2 6 4.7 O=C(O)c1cncc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171011 10728 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 473 6 2 6 4.7 O=C(O)c1cncc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2010.04.142
49798461 10691 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1170725 10691 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57398458 69121 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924013 69121 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.8 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57393220 69124 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924016 69124 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
15985914 83972 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83972 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985914 83972 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83972 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985912 83973 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83973 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
57394938 69116 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924008 69116 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
57394938 69116 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924008 69116 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
49798291 10555 None 0 Mouse Functional pKi = 6 6.0 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169652 10555 None 0 Mouse Functional pKi = 6 6.0 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
49798289 10648 None 0 Mouse Functional pKi = 6 6.0 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10648 None 0 Mouse Functional pKi = 6 6.0 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798289 10648 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10648 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798462 10594 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 463 5 1 5 5.7 O=S(=O)(Nc1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169994 10594 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 463 5 1 5 5.7 O=S(=O)(Nc1cc(Cl)cnc1Oc1cncc(Cl)c1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
44296310 188267 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL49994 188267 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296310 188267 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL49994 188267 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296310 188267 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL49994 188267 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 458 10 2 3 5.4 CN(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
49798289 10648 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10648 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
9870980 154645 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL399472 154645 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
49798265 10726 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10726 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798461 10691 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1170725 10691 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57393218 69115 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924007 69115 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
9870980 154645 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL399472 154645 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296287 101685 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL299379 101685 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
57400125 69112 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 69112 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57400126 69113 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924005 69113 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44296265 194593 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53131 194593 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296265 194593 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53131 194593 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296265 194593 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53131 194593 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 491 10 2 2 7.0 O=C(/C=C/c1ccc(-c2ccccc2)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798463 10595 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 454 5 1 6 4.9 N#Cc1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cn1 10.1016/j.bmcl.2010.04.142
CHEMBL1169995 10595 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 454 5 1 6 4.9 N#Cc1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cn1 10.1016/j.bmcl.2010.04.142
49798289 10648 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170391 10648 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1c(F)cccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798347 10573 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169824 10573 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.04.142
49798323 10786 None 0 Mouse Functional pKi = 6.8 6.8 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171760 10786 None 0 Mouse Functional pKi = 6.8 6.8 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
19430534 10770 None 0 Mouse Functional pKi = 5.8 5.8 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171586 10770 None 0 Mouse Functional pKi = 5.8 5.8 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57396690 69118 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924010 69118 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
57400128 69123 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924015 69123 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(Oc2ccc(C(=O)NCCN3CCCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
44296501 101784 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
CHEMBL300025 101784 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
44296501 101784 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL300025 101784 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296501 101784 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL300025 101784 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 472 8 3 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296264 194592 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.6 CC(C)(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53130 194592 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.6 CC(C)(C)c1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44446951 94602 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL252186 94602 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44446951 94602 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL252186 94602 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 12 2 2 6.7 CCCCc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
49798438 10690 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 429 5 1 5 5.0 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170722 10690 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 429 5 1 5 5.0 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798323 10786 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171760 10786 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798464 10627 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 430 5 1 6 4.4 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170187 10627 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 430 5 1 6 4.4 O=S(=O)(Nc1cc(Cl)cnc1Oc1cccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798264 10785 None 0 Mouse Functional pKi = 5.7 5.7 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10785 None 0 Mouse Functional pKi = 5.7 5.7 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57400129 69125 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924017 69125 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 601 9 2 5 6.4 O=C(NCCN1CCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400125 69112 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924004 69112 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57391450 69117 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924009 69117 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
44296268 101841 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 3 3 6.7 Cc1[nH]c2ccc(O)cc2c1C1CCN(CCCCCNC(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL300455 101841 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 3 3 6.7 Cc1[nH]c2ccc(O)cc2c1C1CCN(CCCCCNC(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(00)00347-4
57393496 69129 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924021 69129 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 629 9 2 5 7.1 Cc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393497 69130 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924022 69130 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 645 10 2 6 6.8 COc1cc(C(=O)NCCN2CCCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
49798437 10557 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169660 10557 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
44296155 101500 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL297950 101500 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296155 101500 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297950 101500 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
57391449 69114 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924006 69114 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
49798264 10785 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10785 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798292 10556 None 0 Mouse Functional pKi = 6.6 6.6 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169653 10556 None 0 Mouse Functional pKi = 6.6 6.6 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798265 10726 None 0 Mouse Functional pKi = 6.6 6.6 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10726 None 0 Mouse Functional pKi = 6.6 6.6 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57391450 69117 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924009 69117 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
44296155 101500 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297950 101500 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 455 7 2 2 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
57394939 69119 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924011 69119 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
44296269 194733 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53557 194733 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296269 194733 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53557 194733 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 440 9 2 3 5.2 N#Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296287 101685 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL299379 101685 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 472 10 3 3 5.3 CC(=O)Nc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
57400127 69122 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924014 69122 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 616 9 2 6 6.2 O=C(NCCN1CCCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
49798436 10702 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1170829 10702 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2010.04.142
49798349 10789 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171786 10789 None 0 Human Functional pKi = 8.5 8.5 - 1
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798399 10698 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1ncccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170801 10698 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1ncccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798265 10726 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10726 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
25110660 94794 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL253424 94794 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
25110660 94794 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL253424 94794 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296630 101363 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL297033 101363 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296630 101363 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297033 101363 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296630 101363 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL297033 101363 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 493 9 2 2 6.1 O=C(/C=C/c1ccc(Br)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296366 189424 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cc(O)ccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL51332 189424 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cc(O)ccc23)CC1 10.1016/s0960-894x(00)00347-4
44296384 194931 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cccc(O)c23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL54192 194931 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3cccc(O)c23)CC1 10.1016/s0960-894x(00)00347-4
49798292 10556 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1169653 10556 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 421 6 2 4 4.8 O=C(O)c1ccccc1Oc1ccc(F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798264 10785 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10785 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798264 10785 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171758 10785 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% human serum
ChEMBL 403 6 2 4 4.6 O=C(O)c1ccccc1Oc1ccccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798397 10696 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1ncncc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170799 10696 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1ncncc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798351 10791 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 341 5 2 4 3.2 CS(=O)(=O)Nc1cc(Cl)ccc1Oc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.142
CHEMBL1171788 10791 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 341 5 2 4 3.2 CS(=O)(=O)Nc1cc(Cl)ccc1Oc1ccccc1C(=O)O 10.1016/j.bmcl.2010.04.142
49798325 10804 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171938 10804 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
57400420 69127 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924019 69127 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57391449 69114 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924006 69114 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 583 9 3 7 4.3 O=C(NCCN1CCNCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
44296087 101653 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299153 101653 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296087 101653 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299153 101653 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296344 162552 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 2 4 6.4 Cn1cc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)c2cc(O)ccc21 10.1016/s0960-894x(00)00347-4
CHEMBL416833 162552 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 9 2 4 6.4 Cn1cc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)c2cc(O)ccc21 10.1016/s0960-894x(00)00347-4
44296087 101653 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299153 101653 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296469 194756 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53779 194756 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296409 194824 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53930 194824 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296469 194756 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53779 194756 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296409 194824 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53930 194824 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296469 194756 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53779 194756 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 471 9 2 2 6.2 O=C(Cc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296409 194824 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53930 194824 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccccc1Cl)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296629 101677 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299322 101677 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296629 101677 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299322 101677 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296629 101677 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299322 101677 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 541 9 2 2 6.0 O=C(/C=C/c1ccc(I)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798350 10790 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 6 2 5 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2010.04.142
CHEMBL1171787 10790 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 443 6 2 5 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)s1 10.1016/j.bmcl.2010.04.142
10436045 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
782 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
CHEMBL432713 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00347-4
10436045 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
782 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
CHEMBL432713 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
49798398 10697 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1cnccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170800 10697 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 438 6 2 5 4.7 O=C(O)c1ccccc1Oc1cnccc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798489 10731 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 434 5 1 6 4.6 Cc1ncccc1Oc1ncc(C#N)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171035 10731 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 434 5 1 6 4.6 Cc1ncccc1Oc1ncc(C#N)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
10436045 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
782 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
CHEMBL432713 3514 None 4 Human Functional pKi = 7.3 7.3 - 1
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2007.12.072
49798325 10804 None 0 Mouse Functional pKi = 6.3 6.3 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171938 10804 None 0 Mouse Functional pKi = 6.3 6.3 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1c(Cl)cccc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
25110679 168150 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
CHEMBL433081 168150 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(00)00347-4
25110679 168150 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL433081 168150 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
25110679 168150 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
CHEMBL433081 168150 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 457 8 2 2 6.3 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2007.12.072
44296428 101759 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL299855 101759 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296428 101759 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299855 101759 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296428 101759 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL299855 101759 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
25110564 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53819 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2Compound was evaluated for the antagonist activity against human C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
25110564 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL53819 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(00)00347-4
25110564 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53819 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
25110564 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL53819 194771 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 465 9 2 2 6.6 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.072
44296398 188288 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL50025 188288 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(00)00347-4
44296398 188288 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL50025 188288 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296410 194717 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53476 194717 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296410 194717 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53476 194717 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296398 188288 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL50025 188288 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1ccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2007.12.072
44296410 194717 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53476 194717 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 449 9 2 2 6.0 O=C(/C=C/c1cccc(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
10940216 191206 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 10 2 3 6.7 COc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
CHEMBL51895 191206 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 513 10 2 3 6.7 COc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
44296077 101882 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL300744 101882 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296077 101882 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL300744 101882 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 485 10 2 2 6.6 O=C(CCc1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44180522 69132 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924024 69132 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 631 10 2 6 6.4 COc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
57393219 69120 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924012 69120 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 581 9 2 5 6.5 O=C(NCCN1CCCCC1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
57393495 69128 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924020 69128 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 637 9 2 5 6.7 O=C(NCCN1CCC(F)(F)C1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.10.038
57400126 69113 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
CHEMBL1924005 69113 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albuminAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs in presence of 5% human serum albumin
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/j.bmcl.2011.10.038
49798265 10726 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171006 10726 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serumAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis in presence of 1% fetal bovine serum
ChEMBL 489 6 2 4 5.8 O=C(O)c1ccccc1Oc1c(F)cc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
49798291 10555 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169652 10555 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 428 6 2 5 4.5 N#Cc1ccc(Oc2ccccc2C(=O)O)c(NS(=O)(=O)c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2010.04.142
49798326 10744 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171207 10744 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
49798326 10744 None 0 Mouse Functional pKi = 6.2 6.2 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171207 10744 None 0 Mouse Functional pKi = 6.2 6.2 - 0
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 417 6 2 4 4.9 Cc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)c(Oc2ccccc2C(=O)O)c1 10.1016/j.bmcl.2010.04.142
44296309 188626 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL50301 188626 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296309 188626 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50301 188626 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296309 188626 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50301 188626 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 431 9 3 3 5.1 O=C(/C=C/c1ccc(O)cc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
9870980 204283 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL71297 204283 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
57394939 69119 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924011 69119 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 568 9 2 6 5.5 O=C(NCCN1CCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
9870980 204283 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL71297 204283 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296154 189152 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL51094 189152 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296154 189152 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL51094 189152 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296154 189152 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL51094 189152 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 469 8 2 2 6.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
49798348 10773 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171614 10773 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 437 6 2 4 5.3 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.142
25110678 194545 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/s0960-894x(00)00347-4
CHEMBL52956 194545 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/s0960-894x(00)00347-4
25110678 194545 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL52956 194545 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
25110678 194545 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
CHEMBL52956 194545 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 467 8 2 2 5.7 O=C(NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.072
44296137 101574 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 576 11 3 4 6.0 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
CHEMBL298562 101574 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 576 11 3 4 6.0 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(CCCCCNC(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1016/s0960-894x(00)00347-4
25110660 154870 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL400698 154870 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
57393218 69115 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924007 69115 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1cccc(Oc2ncc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2011.10.038
15985912 83973 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83973 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83976 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83976 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 0.1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83976 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83976 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serumAntagonist activity at CCR2 assessed as inhibition of CCL2-stimulated THP-1 cell chemotaxis in presence of 1% human serum
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
25110660 154870 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL400698 154870 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2007.12.072
44296628 188713 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL50460 188713 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296266 194851 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/s0960-894x(00)00347-4
CHEMBL53991 194851 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/s0960-894x(00)00347-4
44296628 188713 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50460 188713 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296266 194851 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
CHEMBL53991 194851 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
57396690 69118 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924010 69118 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 582 9 2 6 5.9 O=C(NCCN1CCCCC1)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2011.10.038
49798396 10756 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1nccnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171398 10756 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 439 6 2 6 4.1 O=C(O)c1ccccc1Oc1nccnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
19430534 10770 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
CHEMBL1171586 10770 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 471 6 2 4 5.7 O=C(O)c1ccccc1Oc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.142
44296628 188713 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL50460 188713 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 483 9 2 2 6.4 O=C(/C=C/c1cccc(C(F)(F)F)c1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296266 194851 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
CHEMBL53991 194851 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 429 9 2 2 5.7 Cc1cccc(/C=C/C(=O)NCCCCCN2CCC(c3c[nH]c4ccccc34)CC2)c1 10.1016/j.bmcl.2007.12.072
57397001 69126 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
CHEMBL1924018 69126 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(Oc2ccc(C(=O)NCCN3CCCC3)cc2)c(NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1Cl 10.1016/j.bmcl.2011.10.038
57395221 69131 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
CHEMBL1924023 69131 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrsAntagonist activity at human CCR2 receptor expressed in CHO cells assessed as inhibition of MCP1-induced [35S]-GTPgammaS binding after 3 hrs
ChEMBL 615 9 2 5 6.7 Cc1cc(C(=O)NCCN2CCCC2)ccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.10.038
44296429 194704 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
CHEMBL53402 194704 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against C-C chemokine receptor type 2Antagonist activity against C-C chemokine receptor type 2
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00347-4
44296429 194704 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53402 194704 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
44296429 194704 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
CHEMBL53402 194704 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human CCR2 receptorAntagonist activity at human CCR2 receptor
ChEMBL 415 9 2 2 5.3 O=C(/C=C/c1ccccc1)NCCCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2007.12.072
8921 3136 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Calculated from ng/ml based on a mol weight of ~150kDa.Calculated from ng/ml based on a mol weight of ~150kDa.
Guide to Pharmacology None None None None None
11185 1989 None 42 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
25134303 1989 None 42 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
CHEMBL2178573 1989 None 42 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
DB16066 1989 None 42 Human Functional pIC50 = 8.3 8.3 - 1
Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.
Guide to Pharmacology 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 None
769 824 None 0 Human Functional pIC50 = 7.4 7.4 -28 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
769 824 None 0 Human Functional pIC50 = 7.4 7.4 -28 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
11192346 2022 None 57 Human Functional pIC50 = 8.3 8.3 1 3
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
9032 2022 None 57 Human Functional pIC50 = 8.3 8.3 1 3
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
CHEMBL2029422 2022 None 57 Human Functional pIC50 = 8.3 8.3 1 3
UnclassifiedUnclassified
Guide to Pharmacology 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 24900280
11527661 2019 None 30 Human Functional pIC50 = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
9045 2019 None 30 Human Functional pIC50 = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
CHEMBL1963131 2019 None 30 Human Functional pIC50 = 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 24900329
776 852 None 0 Human Functional pIC50 = 8.5 8.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
759 866 None 0 Human Functional pIC50 = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
759 866 None 0 Human Functional pIC50 = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
759 866 None 0 Human Functional pIC50 = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
11597 673 None 5 Human Functional pIC50 = 8.6 8.6 11 2
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
23725180 673 None 5 Human Functional pIC50 = 8.6 8.6 11 2
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
CHEMBL4781426 673 None 5 Human Functional pIC50 = 8.6 8.6 11 2
UnclassifiedUnclassified
Guide to Pharmacology 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 34141082
46213922 546 None 0 Human Functional pIC50 = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
57656761 546 None 0 Human Functional pIC50 = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
7825 546 None 0 Human Functional pIC50 = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 411 3 2 4 1.8 O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl None
772 869 None 0 Human Functional pIC50 = 8.6 8.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 827 None 0 Human Functional pIC50 = 8.7 8.7 -7 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
770 827 None 0 Human Functional pIC50 = 8.7 8.7 -7 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
68764898 671 None 2 Human Functional pIC50 = 9.2 9.2 3 2
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
9430 671 None 2 Human Functional pIC50 = 9.2 9.2 3 2
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
CHEMBL3577945 671 None 2 Human Functional pIC50 = 9.2 9.2 3 2
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 25893046
771 835 None 0 Human Functional pIC50 = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10770925
771 835 None 0 Human Functional pIC50 = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
771 835 None 0 Human Functional pIC50 = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
771 835 None 0 Human Functional pIC50 = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9276730
771 835 None 0 Human Functional pIC50 = 9.8 9.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9346309
775 848 None 0 Human Functional pIC50 None 6.2 6.2 -316 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15207250
10000456 3387 None 33 Human Functional pIC50 None 6.3 6.3 1 2
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
779 3387 None 33 Human Functional pIC50 None 6.3 6.3 1 2
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
CHEMBL1593104 3387 None 33 Human Functional pIC50 None 6.3 6.3 1 2
UnclassifiedUnclassified
Guide to Pharmacology 390 3 1 3 4.8 O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F 10770925
774 3975 None 0 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12554737
10008367 2020 None 50 Mouse Functional pIC50 None 8 8.0 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
777 2020 None 50 Mouse Functional pIC50 None 8 8.0 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
CHEMBL1289316 2020 None 50 Mouse Functional pIC50 None 8 8.0 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
CHEMBL2426341 2020 None 50 Mouse Functional pIC50 None 8 8.0 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 16210643
773 1935 None 0 Human Functional pIC50 None 8.3 8.3 12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9789057
5071702 3390 None 0 Human Functional pIC50 None 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 2 2.9 Clc1cccc(c1)Cn1cccc1C(=O)O 10770925
780 3390 None 0 Human Functional pIC50 None 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 2 2.9 Clc1cccc(c1)Cn1cccc1C(=O)O 10770925
778 2466 None 0 Human Functional pIC50 None 8.8 8.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600978
486830 4000 None 0 Human Functional pIC50 None 9.1 9.1 6 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217
768 4000 None 0 Human Functional pIC50 None 9.1 9.1 6 5
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9287217


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
183790 3740 None 11 Human Binding pIC50 = 10.5 10.5 -6 2
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3740 None 11 Human Binding pIC50 = 10.5 10.5 -6 2
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 10.5 10.5 -6 2
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
4410 3135 None 106 Human Binding pIC50 = 10.4 10.4 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
65015 3135 None 106 Human Binding pIC50 = 10.4 10.4 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
844 3135 None 106 Human Binding pIC50 = 10.4 10.4 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
CHEMBL18442 3135 None 106 Human Binding pIC50 = 10.4 10.4 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
DB06809 3135 None 106 Human Binding pIC50 = 10.4 10.4 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
183790 3740 None 11 Human Binding pIC50 = 10.1 10.1 -6 2
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3740 None 11 Human Binding pIC50 = 10.1 10.1 -6 2
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 10.1 10.1 -6 2
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
4410 3135 None 106 Human Binding pIC50 = 10.1 10.1 - 1
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
65015 3135 None 106 Human Binding pIC50 = 10.1 10.1 - 1
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
844 3135 None 106 Human Binding pIC50 = 10.1 10.1 - 1
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
CHEMBL18442 3135 None 106 Human Binding pIC50 = 10.1 10.1 - 1
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
DB06809 3135 None 106 Human Binding pIC50 = 10.1 10.1 - 1
Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells
ChEMBL 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 10.1074/jbc.m705302200
68767577 109814 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233186 109814 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
68988296 109816 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233188 109816 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
11627840 95697 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 6.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL258205 95697 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 6.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
68764898 671 None 2 Human Binding pIC50 = 9.6 9.6 - 3
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 671 None 2 Human Binding pIC50 = 9.6 9.6 - 3
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 671 None 2 Human Binding pIC50 = 9.6 9.6 - 3
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
183790 3740 None 11 Human Binding pIC50 = 9.6 9.6 -6 2
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
783 3740 None 11 Human Binding pIC50 = 9.6 9.6 -6 2
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 9.6 9.6 -6 2
Displacement of [125I]MCP1 from CCR2 expressed in CHOK1 cellsDisplacement of [125I]MCP1 from CCR2 expressed in CHOK1 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1074/jbc.m705302200
90656027 111124 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 557 4 1 5 4.6 CNC(=O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263286 111124 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 557 4 1 5 4.6 CNC(=O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
91884571 181458 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4764460 181458 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
46886055 8042 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090893 8042 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
68767577 109814 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233186 109814 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 545 8 1 5 3.7 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
10289827 187974 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187974 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
46886536 8304 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 5 4.7 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092678 8304 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 5 4.7 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
154572822 171099 None 1 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 542 7 2 7 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4457723 171099 None 1 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 542 7 2 7 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
16064151 121237 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 6 1 5 5.2 CC(C)[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577948 121237 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 6 1 5 5.2 CC(C)[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
44425292 85966 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230281 85966 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
68764925 121235 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577946 121235 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
46865775 8112 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
CHEMBL1091605 8112 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
68769744 109815 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 5 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233187 109815 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 5 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(=O)(=O)C(C)C)C1 10.1016/j.bmcl.2014.02.013
11192346 2022 None 57 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of CCR2-mediated Erk phosphorylationInhibition of CCR2-mediated Erk phosphorylation
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
68764925 121235 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577946 121235 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 477 6 1 5 4.9 CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
68767049 121232 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
CHEMBL3577942 121232 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
162668957 182758 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4790208 182758 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
68769143 109812 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233184 109812 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
11643006 95272 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 618 8 3 5 5.3 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL256301 95272 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 618 8 3 5 5.3 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
11540494 95468 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257191 95468 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11598 672 None 9 Human Binding pIC50 = 9.2 9.2 - 1
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
23725177 672 None 9 Human Binding pIC50 = 9.2 9.2 - 1
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL4442783 672 None 9 Human Binding pIC50 = 9.2 9.2 - 1
Inhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assayInhibition of CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 10 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
11598 672 None 9 Human Binding pIC50 = 9.2 9.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
23725177 672 None 9 Human Binding pIC50 = 9.2 9.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4442783 672 None 9 Human Binding pIC50 = 9.2 9.2 - 1
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
68767802 109809 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 506 7 1 6 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233181 109809 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 506 7 1 6 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68764898 671 None 2 Human Binding pIC50 = 9.2 9.2 - 3
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
9430 671 None 2 Human Binding pIC50 = 9.2 9.2 - 3
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL3577945 671 None 2 Human Binding pIC50 = 9.2 9.2 - 3
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
68764898 671 None 2 Human Binding pIC50 = 9.2 9.2 - 3
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 671 None 2 Human Binding pIC50 = 9.2 9.2 - 3
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 671 None 2 Human Binding pIC50 = 9.2 9.2 - 3
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
11597 673 None 5 Human Binding pIC50 = 9.1 9.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
23725180 673 None 5 Human Binding pIC50 = 9.1 9.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4781426 673 None 5 Human Binding pIC50 = 9.1 9.1 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
46865774 8111 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091604 8111 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46886539 8347 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 597 8 1 5 4.5 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092941 8347 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 597 8 1 5 4.5 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46865774 8111 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1091604 8111 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44425294 143363 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389771 143363 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
46865774 8111 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
CHEMBL1091604 8111 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
66767933 121223 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 531 12 6 5 3.2 CCC[C@H](O)[C@H](CNCC(C)(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577933 121223 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 531 12 6 5 3.2 CCC[C@H](O)[C@H](CNCC(C)(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
11192943 77622 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088212 77622 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 628 8 2 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.08.002
68772423 171962 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 541 7 1 7 3.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4470701 171962 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 541 7 1 7 3.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
50925394 19326 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19326 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
22143334 187806 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495924 187806 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 8 4 6 2.7 CSc1ccc(CNC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
68988296 109816 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233188 109816 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 559 7 1 5 4.1 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
11721374 94991 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 604 8 3 5 4.4 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL254772 94991 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 604 8 3 5 4.4 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44448839 155452 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 526 6 3 4 4.7 Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL403889 155452 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 526 6 3 4 4.7 Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44448879 155666 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 527 6 3 4 4.8 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL404904 155666 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 527 6 3 4 4.8 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
46865775 8112 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091605 8112 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
46865775 8112 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
CHEMBL1091605 8112 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2014.02.013
57402219 71006 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71006 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
68767049 121232 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
CHEMBL3577942 121232 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 553 9 3 4 4.9 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NCC)C1=O 10.1021/ml500505q
68867935 109813 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 539 9 1 5 4.0 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(-c3ccccc3)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233185 109813 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 539 9 1 5 4.0 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(-c3ccccc3)c2)C1=O 10.1016/j.bmcl.2014.02.013
11598 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
23725177 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
CHEMBL4442783 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.8b00439
11598 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
23725177 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4442783 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00082
66768099 121222 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 517 13 6 5 2.9 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577932 121222 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 517 13 6 5 2.9 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
69035439 77646 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088388 77646 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 576 7 1 5 5.2 CC(C)N(C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
68767124 109808 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 505 7 1 5 3.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233180 109808 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 505 7 1 5 3.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68769143 109812 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
CHEMBL3233184 109812 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 8 1 5 3.3 CCS(=O)(=O)C[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2014.02.013
89845025 109817 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 575 8 1 6 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233189 109817 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 575 8 1 6 4.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
44593562 187493 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187493 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
46865774 8111 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
CHEMBL1091604 8111 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1021/ml500505q
68768923 109818 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 577 7 1 5 4.3 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233190 109818 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 577 7 1 5 4.3 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)C(C)(C)C)C1 10.1016/j.bmcl.2014.02.013
10240064 188426 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 188426 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
10129192 188457 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL502793 188457 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
91884571 181458 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4764460 181458 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 471 5 3 5 2.5 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(C)(C)C)n2)C1=O 10.1021/acsmedchemlett.1c00082
10144709 166882 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 574 6 2 3 6.7 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL428602 166882 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 574 6 2 3 6.7 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425245 85774 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 608 7 2 5 6.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CCC12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL229316 85774 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 608 7 2 5 6.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CCC12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44425281 153244 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 4 5 6.2 N=C(N)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397749 153244 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 4 5 6.2 N=C(N)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11606411 85306 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226066 85306 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
11598 672 None 9 Human Binding pIC50 = 8.9 8.9 - 1
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1016/j.ejmech.2020.112736
23725177 672 None 9 Human Binding pIC50 = 8.9 8.9 - 1
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1016/j.ejmech.2020.112736
CHEMBL4442783 672 None 9 Human Binding pIC50 = 8.9 8.9 - 1
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1016/j.ejmech.2020.112736
57335017 70336 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70336 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10175425 193531 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526752 193531 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
155531379 171603 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 532 7 1 5 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](N(C)S(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4465351 171603 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 532 7 1 5 2.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](N(C)S(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44454820 97888 None 8 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.016
CHEMBL272369 97888 None 8 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.016
44425293 153462 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397948 153462 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44423283 85305 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226065 85305 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
44593563 193108 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL522688 193108 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44593562 187493 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187493 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
71768865 111120 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 3 0 4 4.8 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 10.1016/j.bmcl.2014.03.036
CHEMBL3263282 111120 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 3 0 4 4.8 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 10.1016/j.bmcl.2014.03.036
162666730 182272 None 1 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pIC50 = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162656188 180913 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4757857 180913 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
24794583 181091 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4760098 181091 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
44425254 142258 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388487 142258 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16066354 121233 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
CHEMBL3577943 121233 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
122178128 121230 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577940 121230 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
42606792 109806 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233178 109806 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
42606792 109806 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL3233178 109806 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44425250 86050 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 630 9 2 5 6.9 CC(=O)Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230790 86050 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 630 9 2 5 6.9 CC(=O)Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 153527 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397996 153527 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
22143255 187856 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL496343 187856 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 523 7 4 6 2.4 CSc1ccc(C(=O)NC2CCN(C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11753466 77638 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088380 77638 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 575 8 2 6 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C#N)cc2)C1 10.1016/j.bmcl.2012.08.002
69035677 77647 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088389 77647 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
155529593 171453 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 518 7 2 5 2.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
CHEMBL4463290 171453 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 minsDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins
ChEMBL 518 7 2 5 2.2 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](NS(C)(=O)=O)C1 10.1021/acsmedchemlett.8b00439
44425652 168766 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168766 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
50925394 19326 None 0 Mouse Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19326 None 0 Mouse Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
52941377 19327 None 0 Mouse Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19327 None 0 Mouse Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
68004034 86580 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315922 86580 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1016/j.bmcl.2012.12.017
76315270 84898 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 576 9 2 7 4.4 CCO[C@@H]1CN([C@H]2CC[C@@](O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CCC(=O)c1cccc(C(F)(F)F)c1 10.1007/s00044-010-9497-9
CHEMBL2236474 84898 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 576 9 2 7 4.4 CCO[C@@H]1CN([C@H]2CC[C@@](O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CCC(=O)c1cccc(C(F)(F)F)c1 10.1007/s00044-010-9497-9
162666730 182272 None 1 Human Binding pIC50 = 8 8.0 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pIC50 = 8 8.0 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
53389845 172959 None 0 Human Binding pIC50 = 8 8.0 - 1
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172959 None 0 Human Binding pIC50 = 8 8.0 - 1
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
11663882 95109 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1cccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1016/j.bmcl.2008.05.010
CHEMBL255500 95109 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1cccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1016/j.bmcl.2008.05.010
11713221 95599 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257768 95599 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11606147 155341 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.7 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL403250 155341 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.7 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44448807 155396 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 558 6 4 4 5.7 O=C(O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL403581 155396 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 558 6 4 4 5.7 O=C(O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
57656715 75204 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036757 75204 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 4.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
70693849 73729 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
CHEMBL2018395 73729 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 491 11 5 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNc1n[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.bmcl.2012.03.007
49763682 65419 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829612 65419 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 489 7 2 4 4.0 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44441352 93381 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 509 7 1 2 6.8 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245686 93381 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 509 7 1 2 6.8 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44441347 93790 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 455 7 1 2 6.1 Cc1ccc(-c2ccc(/C=C/C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)cc2)cc1 10.1016/j.bmcl.2007.01.115
CHEMBL247537 93790 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 455 7 1 2 6.1 Cc1ccc(-c2ccc(/C=C/C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)cc2)cc1 10.1016/j.bmcl.2007.01.115
44425631 142073 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388007 142073 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413089 77905 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 459 8 1 3 5.1 CN(C)CC/C=N/[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209411 77905 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 459 8 1 3 5.1 CN(C)CC/C=N/[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
11319072 74540 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029420 74540 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cncnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
11330837 74549 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029570 74549 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2cc(C(F)(F)F)ncn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
11756884 19087 None 0 Mouse Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19087 None 0 Mouse Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
11562947 89824 None 0 Human Binding pIC50 = 8 8.0 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 544 6 3 4 5.6 O=C(O)C(C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237754 89824 None 0 Human Binding pIC50 = 8 8.0 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 544 6 3 4 5.6 O=C(O)C(C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
12093170 871 None 31 Human Binding pIC50 = 8 8.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
9431 871 None 31 Human Binding pIC50 = 8 8.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL4519152 871 None 31 Human Binding pIC50 = 8 8.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL5268600 193570 None 0 Human Binding pIC50 = 8 8.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C2CCC(O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/acs.jmedchem.6b01309
57395216 71010 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951771 71010 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ncccn3)CC2)C1 10.1021/ml200030q
53322809 58455 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683060 58455 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
53321483 58473 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683078 58473 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
57391766 71015 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951776 71015 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
162658125 181094 None 0 Human Binding pIC50 = 7 7.0 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pIC50 = 7 7.0 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
10184250 73700 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018365 73700 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
10186010 73709 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 513 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)c2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018375 73709 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 513 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)c2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
46241120 83574 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 481 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204258 83574 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 481 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cccs3)CC2)C1 10.1021/ml300260s
44442557 154923 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2(C)CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401010 154923 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2(C)CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
781 3394 None 80 Human Binding pIC50 = 7 7.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
9953769 3394 None 80 Human Binding pIC50 = 7 7.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
CHEMBL134074 3394 None 80 Human Binding pIC50 = 7 7.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
10436045 3514 None 4 Human Binding pIC50 = 7 7.0 -85 13
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
782 3514 None 4 Human Binding pIC50 = 7 7.0 -85 13
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
CHEMBL432713 3514 None 4 Human Binding pIC50 = 7 7.0 -85 13
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
89823342 126357 None 0 Human Binding pIC50 = 7 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650405 126357 None 0 Human Binding pIC50 = 7 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
56680600 65415 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 501 6 2 5 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN(C2CC=C(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829607 65415 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 501 6 2 5 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN(C2CC=C(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44413167 79717 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL211560 79717 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
46842232 7880 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1089965 7880 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
10161975 93958 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248416 93958 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11843945 78050 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 504 8 1 2 6.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL209975 78050 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 504 8 1 2 6.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
5481702 205821 None 1 Human Binding pIC50 = 5 5.0 - 0
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
CHEMBL83338 205821 None 1 Human Binding pIC50 = 5 5.0 - 0
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR2 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
56672021 65613 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 433 5 2 5 3.0 C#C[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1833983 65613 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 433 5 2 5 3.0 C#C[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44453208 169420 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1ccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL442451 169420 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1ccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)cc1 10.1016/j.bmcl.2008.02.015
11329244 71114 None 11 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
CHEMBL195433 71114 None 11 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 486 7 2 5 5.4 CC(=O)c1sc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)nc1C 10.1021/jm049530m
11272103 124373 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
CHEMBL363840 124373 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of C-C chemokine receptor type 2Inhibition of C-C chemokine receptor type 2
ChEMBL 505 7 2 6 4.7 Cn1nnnc1-c1cccc(NC(=O)N[C@@H]2CCCC[C@H]2CN2CCC[C@@H](Cc3ccc(F)cc3)C2)c1 10.1021/jm049530m
44353447 3773 None 0 Human Binding pIC50 = 4 4.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
785 3773 None 0 Human Binding pIC50 = 4 4.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
CHEMBL337246 3773 None 0 Human Binding pIC50 = 4 4.0 - 1
Inhibition of wild type CCR2 mutant (unknown origin)Inhibition of wild type CCR2 mutant (unknown origin)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
11227368 77641 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 618 9 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C3CCCC3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088383 77641 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 618 9 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C3CCCC3)cc2)C1 10.1016/j.bmcl.2012.08.002
25267730 148247 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 5.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)CC1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393632 148247 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 5.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)CC1CCOCC1 10.1016/j.bmcl.2007.01.115
9885683 18945 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 369 3 1 4 3.9 O=C(O)c1cc2ccccc2n1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL128640 18945 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 369 3 1 4 3.9 O=C(O)c1cc2ccccc2n1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823584 126326 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 537 6 1 6 3.8 COc1ccc(N2C[C@@H]3C[C@H]2CN3C(=O)[C@@]23CCC[C@@H]2C[C@@H](N[C@H]2CCOC[C@H]2OC)C3)cc1C(F)(F)F nan
CHEMBL3650376 126326 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 537 6 1 6 3.8 COc1ccc(N2C[C@@H]3C[C@H]2CN3C(=O)[C@@]23CCC[C@@H]2C[C@@H](N[C@H]2CCOC[C@H]2OC)C3)cc1C(F)(F)F nan
162658125 181094 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
44353196 20923 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 343 3 1 4 4.2 Clc1ccc(Cn2c(-c3nn[nH]n3)cc3ccccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL131087 20923 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 343 3 1 4 4.2 Clc1ccc(Cn2c(-c3nn[nH]n3)cc3ccccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
10371682 73813 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018541 73813 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
22310939 115663 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2ccc(C(F)(F)F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL335378 115663 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2ccc(C(F)(F)F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
70681778 75215 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
CHEMBL2036768 75215 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1cccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)c1 10.1016/j.bmcl.2012.04.118
89823498 126311 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
CHEMBL3650361 126311 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
44439169 90772 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239170 90772 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44439169 90772 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239170 90772 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 622 16 1 5 8.8 CCC(C)CC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
49863202 15210 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 550 12 1 4 7.6 CCN(CC)C(C)CCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210670 15210 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 550 12 1 4 7.6 CCN(CC)C(C)CCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71518728 86406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 481 4 1 5 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314065 86406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 481 4 1 5 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44414578 78406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.2 C[C@](CCN1CCC(c2ccccc2)CC1)(CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL211106 78406 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.2 C[C@](CCN1CCC(c2ccccc2)CC1)(CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
11570431 91980 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241502 91980 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44353418 22535 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cccc([N+](=O)[O-])c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL132584 22535 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cccc([N+](=O)[O-])c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71768830 111103 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263261 111103 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
57344302 130645 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 3 4 5.3 CC1(C)Cc2cc(/C=C/C(=O)N3CCC(C(NC4CCC(c5c[nH]c6ccccc56)CC4)C(N)=O)CC3)ccc2O1 nan
CHEMBL3681893 130645 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 3 4 5.3 CC1(C)Cc2cc(/C=C/C(=O)N3CCC(C(NC4CCC(c5c[nH]c6ccccc56)CC4)C(N)=O)CC3)ccc2O1 nan
72663455 129399 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129399 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11753664 77620 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088210 77620 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
10207639 73810 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 4 5 3.7 CCC[C@H](OC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018538 73810 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 4 5 3.7 CCC[C@H](OC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
44595711 137319 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137319 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
53322810 58470 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58470 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11409228 74532 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029412 74532 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
70689914 74550 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74550 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
44453440 97686 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97686 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
10142792 93739 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247245 93739 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
71768689 111109 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263269 111109 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
53319664 58675 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684700 58675 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
23630215 62542 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62542 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
53321482 58459 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683064 58459 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
53318314 58669 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 445 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684692 58669 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 445 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
53323654 58674 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 447 6 1 5 2.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684699 58674 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 447 6 1 5 2.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
72947191 105258 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115275 105258 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
49763574 65442 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829636 65442 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44442532 93483 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246213 93483 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442594 93771 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCc3ccccc3)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247456 93771 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCc3ccccc3)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
10205937 93961 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248419 93961 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
10300282 154775 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 494 10 3 5 2.3 CON(C)C(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400158 154775 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 494 10 3 5 2.3 CON(C)C(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
22310954 24076 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133839 24076 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71518897 86387 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 433 4 1 5 3.0 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313782 86387 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 433 4 1 5 3.0 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44442571 154778 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 508 10 4 5 2.6 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL400160 154778 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 508 10 4 5 2.6 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
11843946 139543 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 490 7 1 2 6.1 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL379624 139543 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 490 7 1 2 6.1 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
11844079 141475 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 580 9 1 2 7.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL384368 141475 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 580 9 1 2 7.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
23655877 169481 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 460 5 3 3 4.7 O=C(O)C(C1CCN(C(=O)Nc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL443058 169481 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 460 5 3 3 4.7 O=C(O)C(C1CCN(C(=O)Nc2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44395113 66115 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 546 8 1 5 5.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL183966 66115 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 546 8 1 5 5.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395058 66331 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 385 7 0 3 4.8 c1ccc(C(CCN2CCCN(Cc3ccncc3)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185032 66331 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 385 7 0 3 4.8 c1ccc(C(CCN2CCCN(Cc3ccncc3)CC2)c2ccccc2)cc1 10.1016/j.bmcl.2004.08.008
18426192 66004 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.1 O=C(CNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL183681 66004 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.1 O=C(CNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
44395093 67124 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 384 8 1 3 4.1 O=C(CCCC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL187476 67124 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 384 8 1 3 4.1 O=C(CCCC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
176 398 None 66 Human Binding pIC50 = 5.0 5.0 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 66 Human Binding pIC50 = 5.0 5.0 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 66 Human Binding pIC50 = 5.0 5.0 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 66 Human Binding pIC50 = 5.0 5.0 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 66 Human Binding pIC50 = 5.0 5.0 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44425322 153199 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL397717 153199 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
89823655 126318 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C)C1 nan
CHEMBL3650368 126318 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C)C1 nan
44444096 93988 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccccc1C1CCN(CC2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248617 93988 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccccc1C1CCN(CC2CCN(C(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44570713 179957 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 580 8 6 6 2.5 CNC(=O)NC1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.12.062
CHEMBL474665 179957 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 580 8 6 6 2.5 CNC(=O)NC1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.12.062
46830335 8213 None 8 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8213 None 8 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
122181150 121836 None 0 Mouse Binding pIC50 = 5.0 5.0 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589845 121836 None 0 Mouse Binding pIC50 = 5.0 5.0 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 608 7 1 3 7.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
49863199 15207 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 528 9 1 4 7.1 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.ejmech.2010.04.024
CHEMBL1210667 15207 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 528 9 1 4 7.1 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.ejmech.2010.04.024
44439158 146825 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
CHEMBL392493 146825 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
46884818 7869 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089881 7869 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
22310877 19541 None 1 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL129958 19541 None 1 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2003.10.049
42632811 93471 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1cccc(NC(=O)c2ccc(Cl)c(Cl)c2)c1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246104 93471 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1cccc(NC(=O)c2ccc(Cl)c(Cl)c2)c1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
127027628 137470 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753826 137470 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(Cl)cc(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
44453373 97809 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271935 97809 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44454793 155090 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL401890 155090 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
23656261 89071 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 485 6 2 3 5.1 Cc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
CHEMBL236510 89071 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 485 6 2 3 5.1 Cc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
53318855 58478 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 COCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683083 58478 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 COCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
44453409 95437 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 95437 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44453441 97687 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271289 97687 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 498 6 3 4 3.2 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
72946982 105227 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115103 105227 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46842086 7977 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1090548 7977 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1cccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
44580424 188024 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 494 8 4 5 4.0 CSc1ccc(CNC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497576 188024 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 494 8 4 5 4.0 CSc1ccc(CNC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11502188 75199 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036752 75199 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10184007 159059 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 3 3 4.6 Cc1cc(C)c(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL409712 159059 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 3 3 4.6 Cc1cc(C)c(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
22310971 20484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2c(C(F)(F)F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130724 20484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2c(C(F)(F)F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22143196 183985 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183985 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
56671923 65737 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834631 65737 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 471 6 3 4 4.5 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
54755079 65739 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
CHEMBL1834633 65739 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 8 4 5 3.5 NC(=O)Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cc1 10.1016/j.bmcl.2011.08.074
54754968 65740 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834634 65740 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 502 7 3 6 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
57400452 70507 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946832 70507 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
57393347 70337 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 623 10 4 6 3.4 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944777 70337 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 623 10 4 6 3.4 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44416138 138872 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138872 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
9850318 95243 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 95243 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
53324942 58676 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684701 58676 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
12093170 871 None 31 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
9431 871 None 31 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
CHEMBL4519152 871 None 31 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
162658125 181094 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53326225 58668 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 431 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684691 58668 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 431 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44583283 188284 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500175 188284 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 714 11 3 8 6.0 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
22143305 183610 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480228 183610 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 3 5 3.2 COc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
12093170 871 None 31 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
9431 871 None 31 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
CHEMBL4519152 871 None 31 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.0c01137
162658125 181094 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pIC50 = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53324943 58682 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 491 6 1 4 3.3 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684707 58682 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 491 6 1 4 3.3 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
57343818 130627 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 524 7 3 3 5.1 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCC3)CC1 nan
CHEMBL3681876 130627 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 524 7 3 3 5.1 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCC3)CC1 nan
86767127 129408 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 7 1.8 COC1COCCC1NC1CC2OC(=O)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671260 129408 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 7 1.8 COC1COCCC1NC1CC2OC(=O)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
56671924 65745 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 491 6 2 5 4.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C4CCCCC4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834639 65745 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 491 6 2 5 4.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C4CCCCC4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44441358 149844 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 427 5 1 3 4.5 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Cl)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL394897 149844 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 427 5 1 3 4.5 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Cl)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
52942863 19247 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 475 6 3 4 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)C2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290186 19247 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 475 6 3 4 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)C2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44442581 93546 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 9 5 5 2.5 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1N 10.1016/j.bmcl.2007.07.028
CHEMBL246410 93546 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 9 5 5 2.5 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1N 10.1016/j.bmcl.2007.07.028
44442555 93724 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 11 4 4 3.6 CCC(C)(C)NC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247203 93724 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 11 4 4 3.6 CCC(C)(C)NC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44442554 93965 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 4 4 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248423 93965 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 4 4 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
11844595 136364 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@]12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL373491 136364 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@]12C=Cc1ccccc12 10.1021/jm060439n
44353395 20091 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 333 3 1 2 5.0 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL130403 20091 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 333 3 1 2 5.0 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1Cl 10.1016/j.bmcl.2003.10.049
11635092 89823 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 5.8 O=C(O)C(C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237753 89823 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 5.8 O=C(O)C(C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
69212799 77974 None 3 Human Binding pIC50 = 5.9 5.9 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL2096789 77974 None 3 Human Binding pIC50 = 5.9 5.9 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
56677296 65418 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1ccc(C(F)(F)F)cc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829611 65418 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1ccc(C(F)(F)F)cc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
25256791 187689 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
CHEMBL495202 187689 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
10143025 93535 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 526 10 4 4 4.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)Nc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246397 93535 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 526 10 4 4 4.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)Nc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444008 155043 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 478 9 1 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL401637 155043 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 478 9 1 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
44395194 64765 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 496 8 1 5 4.1 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL181918 64765 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 496 8 1 5 4.1 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
25008679 94176 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249607 94176 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
24801178 156840 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 481 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL407145 156840 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 481 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NC(=O)c1ccc(Cl)cc1 10.1021/jm701488f
44453329 155349 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL403281 155349 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 2 3 3.5 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
22310903 22612 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c12 10.1016/j.bmcl.2003.10.049
CHEMBL132662 22612 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c12 10.1016/j.bmcl.2003.10.049
76325121 105239 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115115 105239 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344309 130651 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 485 7 3 4 4.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3cccnc32)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3681899 130651 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 485 7 3 4 4.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3cccnc32)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
49863201 15209 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 536 12 1 4 7.2 CCN(CC)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210669 15209 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 536 12 1 4 7.2 CCN(CC)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11663995 146826 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 550 13 1 4 7.6 CCN(CC)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL392494 146826 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 550 13 1 4 7.6 CCN(CC)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11567495 75197 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036750 75197 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10052388 187550 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494541 187550 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1016/j.bmcl.2008.12.050
22143308 187762 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 9 5 6 2.8 CCSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495717 187762 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 9 5 6 2.8 CCSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44573609 187551 None 1 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1007/s00044-010-9501-4
CHEMBL494542 187551 None 1 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1007/s00044-010-9501-4
10256127 73811 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(N)cc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018539 73811 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(N)cc(C(F)(F)F)c2)C1=O 10.1016/j.bmcl.2012.03.007
44353356 117598 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2ccc(-c3ccccc3)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL340072 117598 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2ccc(-c3ccccc3)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
11227383 77645 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 620 11 2 5 6.2 CC(C)CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088387 77645 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 620 11 2 5 6.2 CC(C)CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
71226374 86404 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 437 3 1 4 3.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314061 86404 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 437 3 1 4 3.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
44416066 79785 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 643 8 2 4 5.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)NS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2006.07.011
CHEMBL211923 79785 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 643 8 2 4 5.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)NS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2006.07.011
22310929 168292 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cccc(F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL434059 168292 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cccc(F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71517402 86380 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313774 86380 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
72946204 105250 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 524 5 1 7 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C3COC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115267 105250 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 524 5 1 7 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C3COC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44415904 80428 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214641 80428 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
11329328 74531 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3cccnc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029411 74531 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 490 6 3 5 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3cccnc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44425630 86025 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230617 86025 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44444035 94285 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 2 3 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(O)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL250408 94285 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 2 3 5.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1CCC(c2ccc(O)cc2)CC1 10.1016/j.bmcl.2007.07.065
44353617 19663 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
CHEMBL130065 19663 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
57656942 75037 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2035000 75037 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1ccc(Cl)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
22310953 23963 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cccc(C(F)(F)F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133748 23963 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cccc(C(F)(F)F)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44353170 21413 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 318 3 1 2 4.1 NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131493 21413 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 318 3 1 2 4.1 NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44425650 86128 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231143 86128 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
89853102 111102 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 552 5 1 8 3.5 COC1COCCC1N[C@@H]1C[C@H]2OC(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263260 111102 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 552 5 1 8 3.5 COC1COCCC1N[C@@H]1C[C@H]2OC(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44415903 81148 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215759 81148 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
89823502 126312 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2F)C1 nan
CHEMBL3650362 126312 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2F)C1 nan
56643545 130621 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130621 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
11192346 2022 None 57 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
46947816 65431 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829624 65431 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
56664979 65741 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834635 65741 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 529 6 2 7 4.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56671925 65747 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834640 65747 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 481 7 2 7 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56678508 65799 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834794 65799 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44415899 80072 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213058 80072 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425641 86064 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230832 86064 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413258 77756 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 446 8 1 2 5.5 CN(C)CCC[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209063 77756 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 446 8 1 2 5.5 CN(C)CCC[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44425315 86246 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 536 8 2 5 5.4 CC(=O)Nc1nc(C(CCN2CCCCC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL231252 86246 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 536 8 2 5 5.4 CC(=O)Nc1nc(C(CCN2CCCCC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425319 86333 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231340 86333 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
53318315 58671 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 473 6 1 4 3.4 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684695 58671 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 473 6 1 4 3.4 CC(CC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
54584109 62545 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62545 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
10187492 147788 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147788 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
69285531 121225 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577935 121225 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
10152864 187872 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496432 187872 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425288 86013 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230507 86013 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425304 143365 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389773 143365 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53326721 58491 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683189 58491 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
53326901 58680 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 449 5 1 4 2.9 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684705 58680 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 449 5 1 4 2.9 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57343820 68952 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 nan
CHEMBL1922816 68952 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 nan
57343819 130624 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1 nan
CHEMBL3681873 130624 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(C(F)(F)F)cc2)CC1 nan
57344311 130653 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681900 130653 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
71719764 86383 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313777 86383 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57396832 70333 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 8 2 5 3.1 CN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944773 70333 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 8 2 5 3.1 CN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
53320968 58666 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 403 5 1 4 2.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684689 58666 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 403 5 1 4 2.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44442553 93486 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 CCNC(=O)[C@@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)[C@@H](C)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246221 93486 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 CCNC(=O)[C@@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)[C@@H](C)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
44442595 166406 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCC(C)C)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL427705 166406 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(NCC(C)C)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44444113 94177 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249608 94177 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11606411 85306 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
CHEMBL226066 85306 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125]hMCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1021/jm070166b
72946384 105253 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 546 5 1 8 2.5 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ncccn3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115270 105253 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 546 5 1 8 2.5 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ncccn3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44442583 93548 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1cc(C)c(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246412 93548 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1cc(C)c(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1C 10.1016/j.bmcl.2007.07.028
9890559 66126 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 462 8 0 4 4.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184053 66126 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 462 8 0 4 4.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
11273475 77644 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 10 2 5 5.8 CC(C)Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088386 77644 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 10 2 5 5.8 CC(C)Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
46884898 7715 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7715 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
22310946 20753 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2c([N+](=O)[O-])cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130937 20753 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2c([N+](=O)[O-])cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
57344310 68934 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922794 68934 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
15518124 138424 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 402 5 1 3 5.5 CN(CCN1CCCCC1)c1ccc(-c2nc3cc(Cl)c(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL377432 138424 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 402 5 1 3 5.5 CN(CCN1CCCCC1)c1ccc(-c2nc3cc(Cl)c(Cl)cc3[nH]2)cc1 10.1016/j.bmcl.2006.04.045
44425649 86127 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86127 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
54586021 62541 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62541 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
44570779 183566 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 550 9 4 5 4.0 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480036 183566 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 550 9 4 5 4.0 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
57344299 68954 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 nan
CHEMBL1922818 68954 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 nan
11467577 77640 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 8 2 5 5.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C(C)(C)C)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088382 77640 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 606 8 2 5 5.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(C(C)(C)C)cc2)C1 10.1016/j.bmcl.2012.08.002
44453536 97927 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272542 97927 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
22310899 22690 None 35 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2003.10.049
CHEMBL132725 22690 None 35 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 285 3 1 2 4.0 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2003.10.049
89823629 126319 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650369 126319 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C)cc(C(F)(F)F)c2)C1 nan
60148505 111108 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263268 111108 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
56643545 130621 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130621 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
86767126 129407 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 545 5 1 6 4.1 COC1COCCC1NC1CC2OC(c3ccccc3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671259 129407 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 545 5 1 6 4.1 COC1COCCC1NC1CC2OC(c3ccccc3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
44415880 169337 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 169337 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
57396998 71012 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951773 71012 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml200030q
44425320 86133 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231149 86133 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44453366 158302 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL408908 158302 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
71768794 111101 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 545 5 1 6 4.1 COC1COCCC1N[C@@H]1C[C@H]2OC(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263259 111101 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 545 5 1 6 4.1 COC1COCCC1N[C@@H]1C[C@H]2OC(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44425286 153245 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397750 153245 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44593564 187230 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187230 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
44425258 168905 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 2 6 6.1 CC(=O)Nc1nc(C(CCN2CCN(c3ccccc3C)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438514 168905 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 2 6 6.1 CC(=O)Nc1nc(C(CCN2CCN(c3ccccc3C)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53322299 58672 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 459 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684696 58672 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 459 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
53326226 58684 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684709 58684 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
56675301 65754 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 7 3 5 3.1 CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834647 65754 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 7 3 5 3.1 CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44444110 154839 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4ccc(Cl)c(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400483 154839 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4ccc(Cl)c(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844469 78400 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
CHEMBL211092 78400 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
89823497 126300 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650350 126300 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
56676473 65806 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccn4C)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834850 65806 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccn4C)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444106 94071 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.5 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249010 94071 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.5 O=C(/C=C/c1cccc(C(F)(F)F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44395144 66991 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NCC2CCCN2Cc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186878 66991 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NCC2CCCN2Cc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.08.009
44593563 193108 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193108 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
46884856 8342 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092921 8342 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
89823512 126352 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650400 126352 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
10414966 155116 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ncccn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL402010 155116 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ncccn3)CC2)C1 10.1016/j.bmcl.2007.12.029
89823482 126303 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
CHEMBL3650353 126303 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
70696469 75212 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 372 5 1 4 2.7 COc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036765 75212 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 372 5 1 4 2.7 COc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
44425649 86127 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86127 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
89823499 126306 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C)n2)C1 nan
CHEMBL3650356 126306 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C)n2)C1 nan
44413230 139095 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378658 139095 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 447 8 2 3 4.2 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
89823444 126324 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL3650374 126324 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
44353334 117441 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccccc1Cl 10.1016/j.bmcl.2003.10.049
CHEMBL339842 117441 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2cc(Cl)ccc2n1Cc1ccccc1Cl 10.1016/j.bmcl.2003.10.049
57343917 130628 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 526 7 3 4 4.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCO3)CC1 nan
CHEMBL3681877 130628 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 526 7 3 4 4.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCO3)CC1 nan
54769305 86578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 483 6 2 5 4.6 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315920 86578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 483 6 2 5 4.6 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
68003962 86579 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315921 86579 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2012.12.017
49764446 65438 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829631 65438 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 518 7 3 5 3.1 CN(C)c1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
54755560 65777 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834721 65777 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 495 8 2 7 3.4 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44415922 141681 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL385540 141681 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
24794624 179614 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4742683 179614 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
162657824 181124 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 482 5 3 4 2.9 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4760566 181124 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 482 5 3 4 2.9 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cccc(C(F)(F)F)c2)C1=O 10.1021/acsmedchemlett.1c00082
53326701 58463 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683068 58463 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425633 86039 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230721 86039 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425648 168702 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL436796 168702 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44442590 93770 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247455 93770 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 606 11 6 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
11553489 121219 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 417 11 4 4 2.3 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577929 121219 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 417 11 4 4 2.3 CCC[C@H](O)[C@H](CNCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11497533 89187 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236722 89187 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11541149 146309 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 6 3 4 4.9 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(O)cc23)CC1 10.1021/jm070902b
CHEMBL392097 146309 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 6 3 4 4.9 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(O)cc23)CC1 10.1021/jm070902b
53323664 58689 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684714 58689 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 5 1 4 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
54583187 62572 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782580 62572 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 484 5 2 6 2.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2O)C1 10.1016/j.bmcl.2011.01.034
44425639 86063 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230831 86063 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
54580190 62569 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782577 62569 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54582215 62558 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782566 62558 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54581190 62560 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782568 62560 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
162658125 181094 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
57344216 130629 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3681878 130629 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(C(F)(F)F)c2)CC1 nan
71517241 86377 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313771 86377 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127025460 137327 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 437 4 1 3 5.1 C[C@H]1CC=C(C(=O)NS(=O)(=O)c2ccccc2)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752690 137327 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 437 4 1 3 5.1 C[C@H]1CC=C(C(=O)NS(=O)(=O)c2ccccc2)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
10165716 93552 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 538 10 4 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(SC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246417 93552 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 538 10 4 5 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(SC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442559 93729 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247208 93729 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
44442547 154890 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 3 4 3.2 CCNC(=O)[C@H](CCN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400793 154890 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 11 3 4 3.2 CCNC(=O)[C@H](CCN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
9873546 78035 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL209899 78035 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
22310976 117045 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2c(Cl)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339099 117045 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2c(Cl)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71519050 86390 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 444 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc([N+](=O)[O-])cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313785 86390 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 444 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc([N+](=O)[O-])cc3C2)C1 10.1016/j.bmcl.2012.10.069
44395048 66159 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 495 8 3 6 2.9 NS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184256 66159 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 495 8 3 6 2.9 NS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395062 66696 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185517 66696 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395028 66953 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL186689 66953 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(Cl)cc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395061 66398 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determinedConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determined
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL185180 66398 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determinedConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell; not determined
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
9825735 93762 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247405 93762 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44444032 94106 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 474 10 1 3 6.2 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249183 94106 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 474 10 1 3 6.2 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844467 77909 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.4 CC(C[C@H](CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1)N1CCC(c2ccccc2)CC1 10.1021/jm060439n
CHEMBL209423 77909 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.4 CC(C[C@H](CNCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1)N1CCC(c2ccccc2)CC1 10.1021/jm060439n
44442540 93484 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL246218 93484 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 3 5 2.5 COC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
46886537 8346 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 511 8 1 5 3.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3ccccc3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092940 8346 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 511 8 1 5 3.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3ccccc3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
76321527 105252 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 551 5 1 8 3.1 COC1COCCC1N[C@@H]1C[C@H]2CN(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115269 105252 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 551 5 1 8 3.1 COC1COCCC1N[C@@H]1C[C@H]2CN(c3nccs3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
89823389 126338 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650388 126338 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 nan
71518407 86400 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 435 3 1 3 4.9 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314057 86400 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 435 3 1 3 4.9 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCC1)C2 10.1016/j.bmcl.2012.10.069
10129107 188427 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 9 3 6 3.4 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502248 188427 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 9 3 6 3.4 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44453534 97879 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL272331 97879 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 3 5 2.5 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)ccc1O 10.1016/j.bmcl.2008.02.015
89823621 126317 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
CHEMBL3650367 126317 None 0 Human Binding pIC50 = 6.8 6.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
22143349 184075 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.6 CSc1ccc(C(=O)NC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL482387 184075 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.6 CSc1ccc(C(=O)NC2CCCCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44573411 193263 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL523857 193263 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1007/s00044-010-9501-4
44453620 95534 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257511 95534 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc([N+](=O)[O-])cc2)C1 10.1016/j.bmcl.2008.02.015
44573411 193263 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523857 193263 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 464 6 2 2 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCC2)C1 10.1016/j.bmcl.2008.12.050
70681271 73806 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 13 5 5 3.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018533 73806 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 13 5 5 3.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
69286635 121229 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577939 121229 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
162658125 181094 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
72663455 129399 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129399 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
86767122 129403 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 509 5 1 6 3.1 COC1COCCC1NC1CC2OC(C3CC3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671255 129403 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 509 5 1 6 3.1 COC1COCCC1NC1CC2OC(C3CC3)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
71519226 86374 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 482 5 1 5 3.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313768 86374 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 482 5 1 5 3.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11647276 75205 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036758 75205 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 3 4.3 CC(C)N1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46240584 83578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
CHEMBL2204262 83578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 532 6 3 6 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nc4ccccc4s3)CC2)C1 10.1021/ml300260s
56671795 65797 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834792 65797 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
54754967 77828 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL2092884 77828 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
22143241 183248 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479642 183248 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 510 8 3 4 3.8 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.12.062
44425634 142016 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL387587 142016 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425277 85957 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 674 10 2 5 8.1 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL230165 85957 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 674 10 2 5 8.1 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
44442592 153681 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 5 5 3.3 CNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398134 153681 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 5 5 3.3 CNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
71768688 111097 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263255 111097 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
71768725 111100 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 509 5 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263258 111100 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 509 5 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44571257 191092 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL518772 191092 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 518 9 3 4 4.3 CC(C)c1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
71745103 126360 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650408 126360 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
11512375 154667 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL399617 154667 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
10227655 73711 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 9 5 5 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(C)(C)O)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018377 73711 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 9 5 5 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C(C)(C)O)c(C)c1 10.1016/j.bmcl.2012.03.007
44415958 80497 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
CHEMBL214747 80497 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
44442575 93542 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 570 9 4 4 3.7 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246405 93542 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 570 9 4 4 3.7 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
25010616 94149 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249413 94149 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
25007996 94151 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249415 94151 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844209 81081 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 572 8 1 3 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccsc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL215515 81081 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 572 8 1 3 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccsc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
127028590 137428 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.2 C[C@@]1(c2cccc(C(F)(F)F)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753478 137428 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.2 C[C@@]1(c2cccc(C(F)(F)F)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
89823481 126305 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
CHEMBL3650355 126305 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
89823459 126332 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)cc2C(F)(F)F)C1 nan
CHEMBL3650382 126332 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)cc2C(F)(F)F)C1 nan
89823431 126333 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2C)C1 nan
CHEMBL3650383 126333 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2C)C1 nan
89823495 126339 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
CHEMBL3650389 126339 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
44395256 65467 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 492 8 1 5 4.2 Cc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL183001 65467 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 492 8 1 5 4.2 Cc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
44593554 188686 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL504065 188686 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
90656019 111106 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 546 5 1 7 1.6 COC1COCCC1N[C@@H]1C[C@H]2N(S(C)(=O)=O)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263266 111106 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 546 5 1 7 1.6 COC1COCCC1N[C@@H]1C[C@H]2N(S(C)(=O)=O)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22310943 24512 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2ccc([N+](=O)[O-])cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL134230 24512 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2ccc([N+](=O)[O-])cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
10348168 95459 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 576 6 1 4 6.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(Cl)nn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL257159 95459 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 576 6 1 4 6.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(Cl)nn3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425317 168856 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL438128 168856 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44453330 95500 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257316 95500 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 483 6 2 3 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.02.015
22143225 183563 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CCC(N)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480035 183563 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CCC(N)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
11620726 90638 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238937 90638 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11620726 90638 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238937 90638 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
127025448 137439 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)cc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753563 137439 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)cc2)C1 10.1016/j.bmcl.2015.11.051
54768835 86591 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cccnc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315933 86591 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cccnc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
11192346 2022 None 57 Mouse Binding pIC50 = 7.8 7.8 - 0
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Mouse Binding pIC50 = 7.8 7.8 - 0
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Mouse Binding pIC50 = 7.8 7.8 - 0
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
57656657 75207 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036760 75207 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(C(F)(F)F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
57656641 75220 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036775 75220 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 4 1 4 3.3 CC(C)N1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
53322810 58470 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683075 58470 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
53326721 58491 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683189 58491 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 554 6 2 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(O)C(F)(F)F)C1 10.1016/j.bmcl.2011.01.015
10162844 73712 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 10 5 5 2.7 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018378 73712 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 480 10 5 5 2.7 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
52944966 19038 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
CHEMBL1288324 19038 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
44425316 142357 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL388869 142357 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
53320350 58673 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684697 58673 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
44425646 86098 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231038 86098 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425653 86227 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231246 86227 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44353447 3773 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
785 3773 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
CHEMBL337246 3773 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2007.07.028
53326645 58683 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 477 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684708 58683 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 477 6 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CCC(F)(F)F)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
53324944 58685 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 457 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684710 58685 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 457 5 1 4 3.0 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44425631 142073 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388007 142073 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 564 5 1 2 7.6 CCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
89823661 126342 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650391 126342 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
54583185 62562 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782570 62562 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ncn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
89823581 126359 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650407 126359 None 0 Human Binding pIC50 = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
72663455 129399 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129399 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
71518574 86389 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313784 86389 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11632418 75195 None 1 Human Binding pIC50 = 6.8 6.8 - 1
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 75195 None 1 Human Binding pIC50 = 6.8 6.8 - 1
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46241720 83558 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 501 6 3 6 2.3 N#Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204242 83558 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 501 6 3 6 2.3 N#Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
135981707 65788 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834783 65788 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 556 8 2 6 4.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNC3=NC(Cc4ccccc4)c4ccc(C(F)(F)F)cc43)C2)CC1 10.1016/j.bmcl.2011.08.074
44441359 93679 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 3 4.2 Cc1ccc2c(c1)OCC(C(=O)Nc1ccc(C[N+](C)(C)C3CCOCC3)cc1)=C2 10.1016/j.bmcl.2007.01.115
CHEMBL246933 93679 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 3 4.2 Cc1ccc2c(c1)OCC(C(=O)Nc1ccc(C[N+](C)(C)C3CCOCC3)cc1)=C2 10.1016/j.bmcl.2007.01.115
10206776 154922 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401009 154922 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 10 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22310896 117449 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cc(C(F)(F)F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339851 117449 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 387 3 1 2 5.7 O=C(O)c1cc2cc(C(F)(F)F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
12093170 871 None 31 Human Binding pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
9431 871 None 31 Human Binding pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
CHEMBL4519152 871 None 31 Human Binding pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of CCR2 (unknown origin)Negative allosteric modulation of CCR2 (unknown origin)
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.7b01844
69315675 73809 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 621 14 5 5 5.1 CCC[C@H](O)[C@H](CN(Cc1ccc(C)cc1C)C(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018537 73809 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 621 14 5 5 5.1 CCC[C@H](O)[C@H](CN(Cc1ccc(C)cc1C)C(C)C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
44442570 93734 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 9 4 4 3.4 CC(C)(C)NC(=O)[C@H](CNCc1ccc(Br)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247214 93734 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 9 4 4 3.4 CC(C)(C)NC(=O)[C@H](CNCc1ccc(Br)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
261407 116562 None 59 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 251 3 1 2 3.4 O=C(O)c1cc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2003.10.049
CHEMBL336399 116562 None 59 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 251 3 1 2 3.4 O=C(O)c1cc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2003.10.049
44395104 66697 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CN2CCC(NCCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL185518 66697 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CN2CCC(NCCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
18426157 123899 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 6 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NC2CCCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL362780 123899 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 6 2 3 3.2 Cc1cccc(C(=O)NCC(=O)NC2CCCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
57656887 75210 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036763 75210 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 376 4 1 3 3.4 O=C(Nc1cccc(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
10239671 187909 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL496632 187909 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 543 8 3 6 3.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
44416274 158552 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL409162 158552 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46842085 8235 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 572 10 2 4 4.5 CCCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1092294 8235 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 572 10 2 4 4.5 CCCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
44573450 187521 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL494399 187521 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1007/s00044-010-9501-4
46842381 8234 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 558 9 2 4 4.1 CCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1092293 8234 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 558 9 2 4 4.1 CCc1ccc(C(=O)N2CCC(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
53324139 58457 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683062 58457 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
10346048 78232 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL210606 78232 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
44573450 187521 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494399 187521 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 492 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCCC2)C1 10.1016/j.bmcl.2008.12.050
57344217 130630 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 564 7 3 5 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 nan
CHEMBL3681879 130630 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 564 7 3 5 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OC(F)(F)O3)CC1 nan
72946775 105233 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115109 105233 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46241717 83565 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204249 83565 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 8 3 6 2.9 CCOc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46240484 83577 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204261 83577 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 496 6 3 6 2.8 Cc1cnc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
56662695 65803 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834798 65803 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 520 7 2 7 4.6 CCc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
11669935 58452 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 467 5 1 4 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683055 58452 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 467 5 1 4 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
44425276 151324 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 654 9 2 5 7.8 CC(C)(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL396101 151324 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 654 9 2 5 7.8 CC(C)(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
70689909 74534 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 496 6 3 6 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3nccs3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029414 74534 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 496 6 3 6 2.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3nccs3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
57402219 71006 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71006 None 0 Mouse Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
53321503 58490 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683188 58490 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
54585107 62559 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62559 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
72946205 105240 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 508 5 1 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115116 105240 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 508 5 1 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44453327 95093 None 25 Human Binding pIC50 = 6.8 6.8 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL255408 95093 None 25 Human Binding pIC50 = 6.8 6.8 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
70691783 73699 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018364 73699 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57402124 70521 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 511 8 3 5 2.8 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947041 70521 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 511 8 3 5 2.8 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
10346048 78232 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL210606 78232 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44441356 96702 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 471 5 1 3 4.6 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Br)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL264108 96702 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 471 5 1 3 4.6 C[N+](C)(Cc1ccc(NC(=O)C2=Cc3ccc(Br)cc3OC2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44453327 95093 None 25 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL255408 95093 None 25 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44444111 94115 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249209 94115 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
90656022 111116 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 510 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2cccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263276 111116 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 510 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2cccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
10346048 78232 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL210606 78232 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1021/jm060439n
11670910 88620 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL235657 88620 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
71519225 86373 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 4 1 5 2.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C#N)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313767 86373 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 4 1 5 2.8 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C#N)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49763568 65414 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829606 65414 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44444007 93997 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 2 5.7 O=C(/C=C/c1ccc(F)cc1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248641 93997 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 2 5.7 O=C(/C=C/c1ccc(F)cc1)NCCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
11670910 88620 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL235657 88620 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
122181146 121832 None 0 Mouse Binding pIC50 = 4.8 4.8 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589841 121832 None 0 Mouse Binding pIC50 = 4.8 4.8 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
44439159 91979 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 522 11 1 4 6.8 CN(C)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241501 91979 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 522 11 1 4 6.8 CN(C)CCCCNC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
49863200 15208 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 508 10 1 4 6.4 CN(C)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210668 15208 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 508 10 1 4 6.4 CN(C)CCCCNC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
25268803 151876 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 383 6 1 2 4.2 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2cccc(F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL396571 151876 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 383 6 1 2 4.2 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2cccc(F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL11359 9778 None 0 Human Binding pIC50 = 4.7 4.7 -2 4
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
89823461 126315 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
CHEMBL3650365 126315 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
44425247 166293 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 585 8 2 6 5.7 Cc1ccccc1N1CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CC1 10.1016/j.bmcl.2006.10.059
CHEMBL427110 166293 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 585 8 2 6 5.7 Cc1ccccc1N1CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(N)n2)CC1 10.1016/j.bmcl.2006.10.059
52943756 19288 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19288 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44425320 86133 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231149 86133 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 713 9 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3cccnc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
56643545 130621 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130621 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
44573537 193231 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2Cc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523696 193231 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2Cc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
44573538 193264 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1007/s00044-010-9501-4
CHEMBL523861 193264 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1007/s00044-010-9501-4
57392725 67864 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 467 9 2 3 5.6 O=C(NCCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.013
CHEMBL1910162 67864 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 467 9 2 3 5.6 O=C(NCCCCN1CCC(Cc2ccc(F)cc2)CC1)Nc1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.013
46885213 8458 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8458 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
68004011 86585 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2012.12.017
CHEMBL2315927 86585 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2012.12.017
54769752 86605 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nncc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316210 86605 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nncc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
57344296 68949 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL1922813 68949 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
10278257 73707 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018373 73707 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
10207590 73708 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018374 73708 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
71452241 83566 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204250 83566 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 574 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OCC(F)(F)F)nc3)CC2)C1 10.1021/ml300260s
56657929 65790 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834785 65790 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 485 6 2 5 4.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccccc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56659197 65802 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834797 65802 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 506 6 2 7 4.3 Cc1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
44425637 85985 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230405 85985 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425317 168856 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL438128 168856 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 726 10 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
508869 95438 None 1 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257066 95438 None 1 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 446 7 3 4 3.1 C=Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44442587 93807 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247608 93807 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 611 12 5 5 4.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCc2ccccc2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442593 147198 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL392814 147198 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 549 11 5 5 3.7 CCNc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
10278257 73707 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1021/ml500505q
CHEMBL2018373 73707 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CC(C)C)c(C)c1 10.1021/ml500505q
53322812 58476 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 500 7 1 7 2.3 COC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683081 58476 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 500 7 1 7 2.3 COC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54585109 62571 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782579 62571 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
89823606 126323 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650373 126323 None 0 Human Binding pIC50 = 7.7 7.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
72946982 105227 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115103 105227 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 602 6 1 7 3.8 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344218 68946 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL1922806 68946 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 484 7 3 3 4.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2)CC1 nan
46241719 83585 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 494 6 3 5 2.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(F)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204270 83585 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 494 6 3 5 2.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(F)nc3)CC2)C1 10.1021/ml300260s
46241829 65412 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829603 65412 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
10165042 93551 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(OC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246416 93551 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 3.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(OC(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442556 93725 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 11 5 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)CO)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247204 93725 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 11 5 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)CO)c(C)c1 10.1016/j.bmcl.2007.07.028
90656026 111119 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 527 7 1 7 2.4 COC1COCCC1N(CCCO)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263281 111119 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 527 7 1 7 2.4 COC1COCCC1N(CCCO)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44444001 94510 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 450 8 1 2 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251621 94510 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 450 8 1 2 5.5 O=C(/C=C/c1cc(F)c(F)c(F)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
23441058 66269 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 429 8 0 4 5.3 O=[N+]([O-])c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184688 66269 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 429 8 0 4 5.3 O=[N+]([O-])c1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395160 123806 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 9 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL362340 123806 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 9 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44415973 81053 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215394 81053 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425654 86228 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231247 86228 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44573409 187392 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493575 187392 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1016/j.bmcl.2008.12.050
44573409 187392 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493575 187392 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 450 6 2 2 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCC2)C1 10.1007/s00044-010-9501-4
89823470 126307 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
CHEMBL3650357 126307 None 0 Human Binding pIC50 = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
10153373 172594 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 627 13 2 6 5.4 CCCN(CCC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL448989 172594 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 627 13 2 6 5.4 CCCN(CCC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
86767120 129401 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671253 129401 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
44448915 95070 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 568 7 3 4 5.0 CC(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL255302 95070 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 568 7 3 4 5.0 CC(=O)Nc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
44449054 155189 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 6 2 3 5.6 O=C(/C=C/c1ccc(F)c(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL402442 155189 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 6 2 3 5.6 O=C(/C=C/c1ccc(F)c(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
162666730 182272 None 1 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pIC50 = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA-[R] from wild type human CCR2 expressed in CHO cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
71768722 111110 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 1 5 2.9 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263270 111110 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 1 5 2.9 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
10239991 188445 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 188445 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
10120907 73722 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018388 73722 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 577 12 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCC1 10.1016/j.bmcl.2012.03.007
10007642 19107 None 0 Mouse Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19107 None 0 Mouse Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
89844945 109807 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 518 7 1 6 2.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233179 109807 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 518 7 1 6 2.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)n3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
68767078 121234 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
CHEMBL3577944 121234 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
68768752 121236 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 463 5 1 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](C)C1 10.1021/ml500505q
CHEMBL3577947 121236 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 463 5 1 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](C)C1 10.1021/ml500505q
11756884 19087 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289083 19087 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 533 8 3 5 3.5 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
10007642 19107 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19107 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
9986630 168797 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 641 9 2 5 6.9 CN(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL437552 168797 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 641 9 2 5 6.9 CN(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11627639 94931 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL254355 94931 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC([C@@H](CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
57396999 71016 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951777 71016 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
22143258 183877 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481010 183877 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 522 9 3 5 3.9 CSc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44593555 188782 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL505722 188782 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 642 10 4 6 4.9 CSc1ccc(C(=O)NC2CC(NC(=O)OCc3ccccc3)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
70691785 73725 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018391 73725 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
69285794 121227 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577937 121227 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
122178128 121230 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577940 121230 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 503 9 2 3 5.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CCc2ccccc2)C1 10.1021/ml500505q
11555827 147115 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1cccc2c(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1021/jm070902b
CHEMBL392748 147115 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 555 7 2 4 5.2 COc1cccc2c(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c12 10.1021/jm070902b
42606792 109806 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233178 109806 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSAAntagonist activity at CCR2 in human monocytes assessed as reduction of chemotaxis in presence of 0.1 M BSA
ChEMBL 517 7 1 5 3.0 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
57395218 71008 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951769 71008 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnc3)CC2)C1 10.1021/ml200030q
44425279 142015 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL387583 142015 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11527661 2019 None 30 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2019 None 30 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2019 None 30 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCR2-mediated Erk phosphorylationInhibition of human CCR2-mediated Erk phosphorylation
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
69285794 121227 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577937 121227 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 455 9 2 3 4.6 CCCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
68767078 121234 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
CHEMBL3577944 121234 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 7 1 5 5.0 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(Cl)cc23)C1=O 10.1021/ml500505q
44583282 172693 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172693 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
11597 673 None 5 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
23725180 673 None 5 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
CHEMBL4781426 673 None 5 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00082
11421840 77636 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088379 77636 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 578 9 2 5 5.2 CCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
50992246 58469 None 2 Mouse Binding pIC50 = 8.6 8.6 - 0
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58469 None 2 Mouse Binding pIC50 = 8.6 8.6 - 0
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
50992246 58469 None 2 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58469 None 2 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity to rat CCR2Binding affinity to rat CCR2
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
24794656 180874 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4757452 180874 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
52941377 19327 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19327 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
53326386 58171 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 465 5 1 6 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1681819 58171 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 465 5 1 6 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
44573608 187549 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL494540 187549 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
54771978 86604 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1nccc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316209 86604 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1nccc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
44595711 137319 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxis
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137319 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of chemotaxis
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
24794624 179614 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4742683 179614 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 492 6 3 6 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
57400160 130637 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 3 5.6 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681885 130637 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 3 5.6 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
86767125 129406 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 511 6 1 6 3.5 CCCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
CHEMBL3671258 129406 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 511 6 1 6 3.5 CCCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
44449030 95144 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 543 6 2 3 6.1 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255680 95144 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 543 6 2 3 6.1 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
44449174 95454 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 7 1 4 5.6 CC(=O)OCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257143 95454 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 553 7 1 4 5.6 CC(=O)OCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44448948 155244 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 569 7 2 5 4.9 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL402749 155244 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 569 7 2 5 4.9 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
71517242 86378 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313772 86378 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11226430 73737 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 14 5 5 4.9 CCCNc1cc(NC(=O)CC(=O)N[C@@H](CNCc2ccc(C)cc2C)[C@@H](O)CCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018403 73737 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 14 5 5 4.9 CCCNc1cc(NC(=O)CC(=O)N[C@@H](CNCc2ccc(C)cc2C)[C@@H](O)CCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
49764322 65439 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829632 65439 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 505 7 3 5 3.1 COc1ccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
11502371 153126 None 3 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 153126 None 3 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44425636 85946 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230078 85946 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425629 86024 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230616 86024 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 536 4 1 2 6.8 C[C@H]1CN([C@@H]2CC[C@H](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425241 86026 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230624 86026 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 570 8 2 5 6.4 Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44453407 95435 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257063 95435 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44453442 97688 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271290 97688 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 434 6 3 4 2.7 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
44442599 93647 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93647 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
69285465 121228 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577938 121228 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11699541 146311 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm070902b
CHEMBL392098 146311 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm070902b
11605867 166764 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 507 6 2 3 5.0 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL428378 166764 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 507 6 2 3 5.0 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
54582217 62568 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782576 62568 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 7 1 6 3.7 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
71517576 86367 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313761 86367 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
71518898 86388 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 477 4 1 5 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313783 86388 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 477 4 1 5 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56675302 65755 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 451 8 3 5 3.3 C=CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834648 65755 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 451 8 3 5 3.3 C=CCO[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56669631 65807 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
CHEMBL1834851 65807 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
25268081 93517 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 423 5 1 2 5.7 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCSCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246313 93517 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 423 5 1 2 5.7 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCSCC1 10.1016/j.bmcl.2007.01.115
9934977 166353 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 482 7 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.04.045
CHEMBL427396 166353 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 482 7 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.04.045
44442560 154924 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 11 4 4 2.6 C=CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401011 154924 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 11 4 4 2.6 C=CCNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
11548199 89920 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cellsDisplacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cells
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89920 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cellsDisplacement of [125I]-mouse MCP1 from CCR2 in mouse WEHI265.1 cells
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11548199 89920 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytesDisplacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89920 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytesDisplacement of [125I]-mouse MCP1 from CCR2 in mouse peripheral blood monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
11548199 89920 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytesDisplacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89920 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytesDisplacement of [125I]-rat MCP1 from rat CCR2 receptor in monocytes
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
42632863 93354 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245497 93354 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44444104 94069 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 458 5 0 2 5.8 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249008 94069 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 458 5 0 2 5.8 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
10957890 23092 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 310 3 1 3 3.9 N#Cc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133063 23092 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 310 3 1 3 3.9 N#Cc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
44415992 80607 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215093 80607 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44453300 97434 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL270005 97434 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 451 7 2 4 3.5 CSc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
44441382 153056 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 4.7 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397595 153056 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 4.7 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
11706775 145766 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391668 145766 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11706775 145766 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL391668 145766 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44453562 155652 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404837 155652 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 431 7 3 6 2.0 Nc1ccc([N+](=O)[O-])cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
56678640 65756 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 7 4 6 1.7 CS(=O)(=O)N[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834650 65756 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 7 4 6 1.7 CS(=O)(=O)N[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54768836 86594 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 508 6 2 6 4.5 N#Cc1ccccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315936 86594 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 508 6 2 6 4.5 N#Cc1ccccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
72947193 105229 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115105 105229 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10585 1078 None 1 Human Binding pIC50 = 7.7 7.7 - 1
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Binding pIC50 = 7.7 7.7 - 1
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Binding pIC50 = 7.7 7.7 - 1
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
57401954 68957 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 nan
CHEMBL1922822 68957 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)c(F)c2)CC1 nan
57656871 75225 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036780 75225 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 3 2 4 2.0 CCN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
49764447 65420 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829613 65420 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755801 65758 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834652 65758 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 559 8 3 8 3.7 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
24801525 97607 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97607 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22143104 188056 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497780 188056 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
44573488 187677 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1007/s00044-010-9501-4
CHEMBL495165 187677 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1007/s00044-010-9501-4
71517575 86386 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313780 86386 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 497 5 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](OC)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49764700 65436 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 493 6 3 4 3.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829629 65436 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 493 6 3 4 3.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
127025461 137383 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 348 3 2 2 4.0 C[C@@]1(c2ccc(Cl)c(C(F)(F)F)c2)C[C@@H](CO)CC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753161 137383 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 348 3 2 2 4.0 C[C@@]1(c2ccc(Cl)c(C(F)(F)F)c2)C[C@@H](CO)CC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
11692057 145487 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 516 7 2 5 4.7 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc([N+](=O)[O-])cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL391460 145487 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 516 7 2 5 4.7 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc([N+](=O)[O-])cc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656585 147629 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL393135 147629 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44444009 93998 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 424 10 1 3 5.0 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248642 93998 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 424 10 1 3 5.0 COc1ccc(C2CCN(CCCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
23441036 67209 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(O)cc3)c3ccc(O)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187856 67209 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 510 8 3 7 3.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(O)cc3)c3ccc(O)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
24801180 98038 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 98038 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
11577400 58453 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 535 5 1 4 5.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683056 58453 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 535 5 1 4 5.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
71768899 111122 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1ccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)cc1 10.1016/j.bmcl.2014.03.036
CHEMBL3263284 111122 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1ccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)cc1 10.1016/j.bmcl.2014.03.036
44415927 80853 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215271 80853 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
11364218 73802 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1OC 10.1016/j.bmcl.2012.03.007
CHEMBL2018529 73802 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1OC 10.1016/j.bmcl.2012.03.007
24801179 156638 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL406925 156638 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
10458152 77799 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209267 77799 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
4485 69377 None 118 Human Binding pIC50 = 5.7 5.7 -1 8
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
CHEMBL193 69377 None 118 Human Binding pIC50 = 5.7 5.7 -1 8
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
68003782 86581 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315923 86581 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1016/j.bmcl.2012.12.017
68004010 86584 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 548 7 3 8 4.3 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
CHEMBL2315926 86584 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 548 7 3 8 4.3 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
71530223 86370 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313764 86370 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49764196 65440 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829633 65440 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 519 6 3 6 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
44573487 192632 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL521697 192632 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1016/j.bmcl.2008.12.050
53320171 58474 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683079 58474 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
72948000 105222 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115099 105222 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67774351 130636 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 3 5.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681884 130636 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 3 5.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
46241827 83562 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 7 3 6 2.8 COc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1C 10.1021/ml300260s
CHEMBL2204246 83562 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 520 7 3 6 2.8 COc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1C 10.1021/ml300260s
10458152 77799 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1021/jm060439n
CHEMBL209267 77799 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccccc1 10.1021/jm060439n
44353396 115247 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 313 3 1 2 4.7 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1C 10.1016/j.bmcl.2003.10.049
CHEMBL334766 115247 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 313 3 1 2 4.7 Cc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1C 10.1016/j.bmcl.2003.10.049
10203447 154626 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL399328 154626 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
10203447 154626 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL399328 154626 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444103 94034 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 470 5 0 2 6.4 Cc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248814 94034 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 470 5 0 2 6.4 Cc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
90656020 111107 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 602 6 1 7 3.9 COC1COCCC1N[C@@H]1C[C@H]2N(C(=O)OCc3ccccc3)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263267 111107 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 602 6 1 7 3.9 COC1COCCC1N[C@@H]1C[C@H]2N(C(=O)OCc3ccccc3)CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22310839 21739 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131885 21739 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823443 126341 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
CHEMBL3650390 126341 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
44395097 67064 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CCNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL187237 67064 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CCNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44442541 154818 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
CHEMBL400382 154818 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)NCc1ccc(C)cc1C 10.1016/j.bmcl.2007.07.028
44439155 91972 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241497 91972 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
53317526 58471 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 470 5 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683076 58471 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 470 5 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
46842235 7834 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089629 7834 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(C(F)(F)F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
44453298 155237 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402723 155237 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 421 6 3 4 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44570780 184043 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.0 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL482201 184043 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 508 7 4 5 3.0 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44425649 86127 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86127 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425305 86062 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 555 8 1 4 6.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2006.10.059
CHEMBL230828 86062 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 555 8 1 4 6.9 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1cscn1 10.1016/j.bmcl.2006.10.059
69285465 121228 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577938 121228 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 457 9 2 4 3.5 COCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
68003997 86598 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 6 3 8 3.6 N#Cc1cc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315940 86598 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 6 3 8 3.6 N#Cc1cc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
57344298 68950 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 nan
CHEMBL1922814 68950 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(F)c2)CC1 nan
71517240 86376 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313770 86376 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56659295 65808 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834852 65808 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 503 7 2 7 4.2 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4noc5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425318 150309 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL395289 150309 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44442586 93809 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247621 93809 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 9 5 5 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442588 93916 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248188 93916 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 577 12 5 5 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NCC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
24801526 97614 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
CHEMBL270959 97614 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 541 7 5 6 1.5 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(S(N)(=O)=O)cc1 10.1021/jm701488f
72947413 105254 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115271 105254 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344229 130638 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681886 130638 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
54755562 65785 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 549 8 2 7 4.0 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC(F)(F)F)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834780 65785 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 549 8 2 7 4.0 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(CC(F)(F)F)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
25268440 93905 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL248153 93905 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 373 5 1 2 4.3 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44573651 187207 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492376 187207 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1016/j.bmcl.2008.12.050
10276594 93963 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 9 4 4 2.1 CNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248420 93963 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 9 4 4 2.1 CNC(=O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
15290299 22614 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL132664 22614 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 319 3 1 2 4.7 O=C(O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22310883 116738 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337485 116738 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44573699 187672 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL495151 187672 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44395029 127286 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL365854 127286 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44444002 93994 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 410 9 1 3 4.6 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248638 93994 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 410 9 1 3 4.6 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2007.07.065
22310869 19471 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
CHEMBL129833 19471 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2cc(C(=O)O)n(Cc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2003.10.049
183790 3740 None 11 Mouse Binding pIC50 = 4.6 4.6 - 2
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3740 None 11 Mouse Binding pIC50 = 4.6 4.6 - 2
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3740 None 11 Mouse Binding pIC50 = 4.6 4.6 - 2
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
44415939 140131 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL380190 140131 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425638 153532 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398001 153532 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44415996 80041 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
CHEMBL212939 80041 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
53317527 58479 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 526 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C2CCOC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683084 58479 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 526 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C2CCOC2)C1 10.1016/j.bmcl.2011.01.015
71518406 86399 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 421 3 1 3 4.5 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314056 86399 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 421 3 1 3 4.5 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCC1)C2 10.1016/j.bmcl.2012.10.069
89823349 126314 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
CHEMBL3650364 126314 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
44593562 187493 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL494191 187493 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1007/s00044-010-9501-4
44453370 155741 None 1 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL405632 155741 None 1 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)N[C@@H]2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2008.02.015
44573538 193264 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523861 193264 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 526 6 2 2 6.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc3C2)C1 10.1016/j.bmcl.2008.12.050
11606167 90948 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239359 90948 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11606167 90948 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239359 90948 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 526 14 1 5 6.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(OC)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71519381 86371 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313765 86371 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 (unknown origin) assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
86767124 129405 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 6 2.7 COC1COCCC1NC1CC2OC(C)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671257 129405 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 483 4 1 6 2.7 COC1COCCC1NC1CC2OC(C)CC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11489078 73803 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018530 73803 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 509 12 4 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(OC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44447815 155036 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 592 6 2 5 6.0 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cc(Cl)ncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL401608 155036 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 592 6 2 5 6.0 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cc(Cl)ncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
53320350 58673 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684697 58673 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 463 6 1 5 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
10162782 73704 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL2018370 73704 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11180885 73733 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018399 73733 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
49763575 65443 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829637 65443 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
44444112 154840 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400484 154840 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 454 7 1 3 5.2 COc1ccc(C2CCN(CC3CCC(NC(=O)/C=C/c4cc(F)cc(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44449204 95707 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 581 8 3 3 5.4 CCNC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL258252 95707 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 581 8 3 3 5.4 CCNC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44395222 67042 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187126 67042 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 512 8 2 6 3.8 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
10279914 73702 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018368 73702 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
44453369 97766 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 3.1 O=C(CNC(=O)c1cccc(Cl)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL271726 97766 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 3.1 O=C(CNC(=O)c1cccc(Cl)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
122181144 121830 None 0 Mouse Binding pIC50 = 4.6 4.6 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589839 121830 None 0 Mouse Binding pIC50 = 4.6 4.6 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 514 6 1 3 5.7 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
8447 188947 None 84 Human Binding pIC50 = 5.6 5.6 -12 13
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188947 None 84 Human Binding pIC50 = 5.6 5.6 -12 13
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
44415900 79934 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 589 8 2 4 4.7 CS(=O)(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL212542 79934 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 589 8 2 4 4.7 CS(=O)(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
3117 207839 None 103 Human Binding pIC50 = 5.6 5.6 -2 16
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207839 None 103 Human Binding pIC50 = 5.6 5.6 -2 16
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
71517737 86369 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313763 86369 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127027956 137578 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 294 2 1 1 4.8 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c2ccccc12 10.1016/j.bmcl.2015.11.051
CHEMBL3754764 137578 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 294 2 1 1 4.8 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c2ccccc12 10.1016/j.bmcl.2015.11.051
69285531 121225 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577935 121225 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 441 8 2 3 4.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
57344303 68929 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922789 68929 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344305 68937 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922797 68937 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
46944853 65428 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829621 65428 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
56677288 65441 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829634 65441 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 6 3 5 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccc4c(c3)OCC4)CC2)C1 10.1016/j.bmcl.2011.06.080
44416157 80593 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80593 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44413257 77439 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 464 8 1 3 5.4 CN(C)CCS[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL208685 77439 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 464 8 1 3 5.4 CN(C)CCS[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
11670968 169373 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL442085 169373 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
54585108 62561 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782569 62561 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
89823348 126346 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650395 126346 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
46241609 83564 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml300260s
CHEMBL2204248 83564 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml300260s
25268085 93904 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Br)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL248151 93904 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2cccc(Br)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
10227556 93964 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 9 3 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248421 93964 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 9 3 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
89823555 126298 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650348 126298 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823534 126299 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650349 126299 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@H]3C[C@@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823347 126328 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncccc2C(F)(F)F)C1 nan
CHEMBL3650378 126328 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncccc2C(F)(F)F)C1 nan
89834736 126336 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@H]1NC1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
CHEMBL3650386 126336 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 1 6 3.6 CO[C@@H]1COCC[C@H]1NC1C[C@H]2CCC[C@@]2(C(=O)N2[C@H]3CC[C@@H]2CN(c2cc(C(F)(F)F)ccn2)C3)C1 nan
53326900 58663 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 425 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(C)C)(N2CCN(C(=O)OC(C)(C)C)CC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684682 58663 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 425 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(C)C)(N2CCN(C(=O)OC(C)(C)C)CC2)C1 10.1016/j.bmcl.2011.01.052
127025447 137532 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 306 3 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3754334 137532 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 306 3 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(-c3ccccc3)c2)C1 10.1016/j.bmcl.2015.11.051
42632888 93629 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 433 6 1 2 5.4 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246725 93629 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 433 6 1 2 5.4 C[N+](C)(Cc1ccc(NC(=O)/C=C/c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
57656729 75224 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 3 1 4 2.4 CCN1CCOC(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036779 75224 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 414 3 1 4 2.4 CCN1CCOC(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44593564 187230 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187230 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
70688149 75222 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036777 75222 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 4 2 4 2.8 CC(C)N1CCN[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44453472 155536 None 1 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155536 None 1 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44425635 153530 None 0 Mouse Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398000 153530 None 0 Mouse Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10196988 169463 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL442929 169463 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 628 10 4 6 4.8 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
44442562 93731 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 9 3 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247210 93731 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 9 3 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
44353464 20897 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1c(Cl)c2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL131065 20897 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1c(Cl)c2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
56661559 65748 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 453 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834641 65748 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 453 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444003 93995 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 1 3 5.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248639 93995 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 9 1 3 5.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44395195 171367 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 490 10 3 5 4.1 Cc1csc(C(=O)NNC(=O)CN2CCCC2CNCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL446178 171367 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 490 10 3 5 4.1 Cc1csc(C(=O)NNC(=O)CN2CCCC2CNCCC(c2ccccc2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.009
71517403 86381 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313775 86381 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 535 4 1 5 4.1 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](C(F)(F)F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
127025728 137534 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1 10.1016/j.bmcl.2015.11.051
CHEMBL3754349 137534 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1 10.1016/j.bmcl.2015.11.051
67774360 130626 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 557 7 4 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL3681875 130626 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 557 7 4 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 nan
44453563 95087 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 430 6 2 4 2.7 N#Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL255385 95087 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 430 6 2 4 2.7 N#Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
57656869 75219 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036774 75219 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 4 1 4 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@H]2CN(C3CC3)CCO2)CC1 10.1016/j.bmcl.2012.04.118
24801180 98038 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 98038 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
68004012 86583 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
CHEMBL2315925 86583 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2012.12.017
183790 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2020.112311
783 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2020.112311
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2020.112311
72947595 105219 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115096 105219 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
183790 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
783 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1007/s00044-010-9497-9
183790 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
783 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm300682j
57656640 75209 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
CHEMBL2036762 75209 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
10208946 73716 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.2 CCCC(O)(CCC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018382 73716 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.2 CCCC(O)(CCC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46241718 83569 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
CHEMBL2204253 83569 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 546 8 3 6 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccc(OC4CCC4)nc3)CC2)C1 10.1021/ml300260s
49763931 65424 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829617 65424 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 499 6 3 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc4[nH]cnc4c3)CC2)C1 10.1016/j.bmcl.2011.06.080
54754723 65751 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834644 65751 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 8 2 6 3.4 CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
54755081 65775 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834719 65775 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57396901 70522 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 9 3 5 3.2 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947042 70522 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 525 9 3 5 3.2 CCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44425650 86128 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231143 86128 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 570 9 1 2 8.3 CCCCCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
183790 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Displacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysisDisplacement of [125I]RANTES from human CCR2 expressed in CHO cells after 40 mins by scintillation counting analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
71768864 111111 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263271 111111 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 5 1 7 2.2 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(OC(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
183790 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
783 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.9b01701
183790 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
783 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Inhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cellsInhibitory effect on the binding of [125I]- MCP-1 to C-C chemokine receptor type 2-expressing CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm9906264
10175423 188444 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502515 188444 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 10 4 6 4.4 CCNC(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
53325639 58468 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683073 58468 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
53321484 58475 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683080 58475 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
44573651 187207 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1007/s00044-010-9501-4
CHEMBL492376 187207 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 508 6 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(C)C)C1 10.1007/s00044-010-9501-4
57344297 68951 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 nan
CHEMBL1922815 68951 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 502 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccccc2F)CC1 nan
46240381 83572 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
CHEMBL2204256 83572 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
44353223 116508 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 329 4 2 3 3.7 O=C(O)c1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL336143 116508 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 329 4 2 3 3.7 O=C(O)c1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
46886508 8315 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 620 8 3 6 6.2 CSc1ccc(CN[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092739 8315 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 620 8 3 6 6.2 CSc1ccc(CN[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
89823438 126329 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C(F)(F)F)cn2)C1 nan
CHEMBL3650379 126329 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C(F)(F)F)cn2)C1 nan
89823624 126330 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 474 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(Cl)c2)C1 nan
CHEMBL3650380 126330 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 474 5 1 6 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(Cl)c2)C1 nan
89823464 126350 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
CHEMBL3650399 126350 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2C#N)C1 nan
89823401 126354 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 512 5 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
CHEMBL3650402 126354 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 512 5 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(Cl)c2C#N)C1 nan
44425638 153532 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398001 153532 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 620 9 1 2 9.2 CCCCCCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
72946381 105234 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115110 105234 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
68616341 73731 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018397 73731 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
56678507 65798 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834793 65798 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44416138 138872 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138872 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
22143196 183985 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183985 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44425642 142344 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388675 142344 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53325385 58456 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683061 58456 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@@H]2C)C1 10.1016/j.bmcl.2011.01.015
53326242 58686 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 452 4 2 4 2.7 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)NC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684711 58686 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 452 4 2 4 2.7 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)NC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
54584164 62566 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782574 62566 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44425649 86127 None 0 Mouse Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86127 None 0 Mouse Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
183790 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
783 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.6 7.6 -6 2
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmcl.2008.12.050
10323468 187670 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1016/j.bmcl.2008.12.050
CHEMBL495149 187670 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1016/j.bmcl.2008.12.050
10119551 93810 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 5 6 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(OC(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247622 93810 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 5 6 2.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(OC(F)(F)F)ccc2N)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22143196 183985 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183985 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
89823620 126361 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650409 126361 None 0 Human Binding pIC50 = 7.6 7.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44425243 85801 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 610 8 2 7 6.2 Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL229536 85801 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 610 8 2 7 6.2 Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44416041 80430 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL214647 80430 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
22310991 19480 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL129881 19480 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395138 123975 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 8 4 7 2.5 O=C(CN1CCCN(CCC(O)(c2ccccc2)c2cccc(O)c2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
CHEMBL362889 123975 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 8 4 7 2.5 O=C(CN1CCCN(CCC(O)(c2ccccc2)c2cccc(O)c2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
70683355 73814 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018542 73814 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 620 11 4 6 5.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)C1=O 10.1016/j.bmcl.2012.03.007
91754543 126364 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 465 4 1 4 4.1 O=C(N1CCN(c2ccc(C(F)(F)F)cc2)CC1)C12CCCC1CC(NC1CCOCC1)C2 nan
CHEMBL3650412 126364 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 465 4 1 4 4.1 O=C(N1CCN(c2ccc(C(F)(F)F)cc2)CC1)C12CCCC1CC(NC1CCOCC1)C2 nan
46241121 83570 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 466 6 3 6 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ncco3)CC2)C1 10.1021/ml300260s
CHEMBL2204254 83570 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 466 6 3 6 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ncco3)CC2)C1 10.1021/ml300260s
49863167 15203 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 561 9 2 6 5.6 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210603 15203 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 561 9 2 6 5.6 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
46886059 7980 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 565 7 1 5 4.0 CN(C)[C@@H]1CC[C@H](N2CCC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090561 7980 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 565 7 1 5 4.0 CN(C)[C@@H]1CC[C@H](N2CCC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
127025446 137278 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752224 137278 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44439156 91973 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 575 10 2 6 5.9 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241498 91973 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 575 10 2 6 5.9 COC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44415903 81148 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215759 81148 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 8 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccccc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
46842084 7913 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1090206 7913 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 544 8 2 4 3.9 Cc1ccccc1C(=O)N1CCC(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
72946387 105224 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115100 105224 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
54756038 65776 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834720 65776 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 468 7 2 7 3.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3noc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56683044 65800 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834795 65800 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 521 6 3 8 3.4 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56659196 65801 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834796 65801 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 522 8 3 8 3.4 O=C(CNc1nn(CCO)c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
71768830 111103 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263261 111103 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 485 4 1 6 3.0 COC1COCCC1N[C@@H]1C[C@H]2SCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
54582216 62563 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782571 62563 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 500 6 1 8 2.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nncc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44573486 193156 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL523054 193156 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1007/s00044-010-9501-4
11721085 166857 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL428559 166857 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
71519055 86396 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 476 4 1 4 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314053 86396 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 476 4 1 4 3.7 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Br)cc3C2)C1 10.1016/j.bmcl.2012.10.069
56668306 65715 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 2 4 5.2 O=C(CSc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834580 65715 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 2 4 5.2 O=C(CSc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
44441396 93581 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 419 5 1 1 6.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246522 93581 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 419 5 1 1 6.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCCC1 10.1016/j.bmcl.2007.01.115
57402254 70510 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946835 70510 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44444109 94114 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 504 6 0 2 7.2 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CCN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL249208 94114 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 504 6 0 2 7.2 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CCN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44443996 155000 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL401387 155000 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
53322813 58480 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 547 7 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](Cc2cccnc2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683085 58480 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 547 7 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](Cc2cccnc2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
127028588 137432 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2cccc(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3753509 137432 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2cccc(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
44415996 80041 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
CHEMBL212939 80041 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 586 8 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)Cc1ccccc1 10.1016/j.bmcl.2006.07.011
24794656 180874 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4757452 180874 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 450 4 3 6 2.0 CC(=O)N[C@@H]1C[C@H](N)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
86767121 129402 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 438 3 1 4 3.3 O=C(N1CCc2ccc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
CHEMBL3671254 129402 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 438 3 1 4 3.3 O=C(N1CCc2ccc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
162656188 180913 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4757857 180913 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 429 5 3 5 1.4 CN[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
44447766 166876 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL428594 166876 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2007.12.029
50992246 58469 None 2 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58469 None 2 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
50992246 58469 None 2 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1683074 58469 None 2 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
25110788 85958 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230166 85958 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425252 142255 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 652 9 2 7 6.6 CC(=O)Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388486 142255 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 652 9 2 7 6.6 CC(=O)Nc1nc(C(CCN2CCC(n3cnc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425255 168882 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438304 168882 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
50992246 58469 None 2 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683074 58469 None 2 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44593563 193108 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193108 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
68769802 121238 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 7 1 6 4.2 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
CHEMBL3577949 121238 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 493 7 1 6 4.2 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/ml500505q
11433008 77635 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088378 77635 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 564 8 2 5 4.9 Cc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
44570781 192563 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL521275 192563 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 515 8 4 4 3.7 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc3[nH]ccc3c2)C1 10.1016/j.bmcl.2008.12.062
44425645 86080 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86080 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53318853 58454 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683059 58454 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 481 5 1 4 4.6 CC(C)[C@]1(C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2011.01.015
53317041 58687 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 465 5 1 5 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684712 58687 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 465 5 1 5 3.3 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC2CCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
53325460 58492 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58492 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
57395217 71007 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951768 71007 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccccn3)CC2)C1 10.1021/ml200030q
57391767 71017 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
CHEMBL1951779 71017 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 534 8 3 6 3.3 CCOc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200030q
53317028 58681 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 493 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684706 58681 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 493 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
25022597 95337 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 95337 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
66768640 121224 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577934 121224 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
16066354 121233 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
CHEMBL3577943 121233 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 567 9 3 4 5.2 CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)C1=O 10.1021/ml500505q
44425644 86079 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230932 86079 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11353855 74547 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74547 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
70689915 74551 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
CHEMBL2029572 74551 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 611 6 3 9 3.3 O=C(N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1)C1(O)CCN(c2cc(C(F)(F)F)ccn2)CC1 10.1021/ml200199c
10117480 73714 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018380 73714 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
53325460 58492 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683190 58492 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 538 6 1 6 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(F)(F)F)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
22143155 188060 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL497788 188060 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
57656833 75227 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75227 None 0 Human Binding pIC50 = 8.5 8.5 - 1
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46886538 8316 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 647 8 1 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1092748 8316 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 647 8 1 5 5.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
44425653 86227 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231246 86227 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 546 6 1 3 6.7 CSC[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425272 86033 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 626 10 2 5 7.2 CCC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230684 86033 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 626 10 2 5 7.2 CCC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425290 153529 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397997 153529 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 628 9 2 6 7.0 COC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53323653 58670 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 475 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
CHEMBL1684694 58670 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 475 5 1 5 3.3 CC(OC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2)C1)C(F)(F)F 10.1016/j.bmcl.2011.01.052
44425644 86079 None 0 Mouse Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230932 86079 None 0 Mouse Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 514 5 1 2 6.7 CCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10281316 73720 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1021/jm300682j
CHEMBL2018386 73720 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1021/jm300682j
10281316 73720 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
CHEMBL2018386 73720 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NCC 10.1016/j.bmcl.2012.03.007
11353843 74545 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029566 74545 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 594 6 2 7 4.8 O=C(C1CCN(c2cccc(C(F)(F)F)c2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
24801690 98039 None 25 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98039 None 25 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
11527661 2019 None 30 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
9045 2019 None 30 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
CHEMBL1963131 2019 None 30 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200030q
10218403 187908 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL496630 187908 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
11527661 2019 None 30 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9045 2019 None 30 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL1963131 2019 None 30 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
70683350 73724 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018390 73724 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
11179439 73734 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018400 73734 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44583280 172447 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 172447 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
44570714 189792 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL516224 189792 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 565 9 5 6 3.6 CSc1ccc(C(=O)NC2CCC(NC(C)C)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
22143112 188443 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
CHEMBL502513 188443 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 594 11 5 6 3.7 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC)C1 10.1016/j.bmcl.2008.07.123
50992246 58469 None 2 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683074 58469 None 2 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
24794585 179522 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4741305 179522 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
44425647 86099 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86099 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425273 86052 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 638 10 2 5 7.2 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)C1CC1 10.1016/j.bmcl.2006.10.059
CHEMBL230794 86052 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 638 10 2 5 7.2 O=C(Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)C1CC1 10.1016/j.bmcl.2006.10.059
162666730 182272 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
44449031 95696 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL258204 95696 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
10323427 79758 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 in human monocytesBinding affinity to CCR2 in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79758 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 in human monocytesBinding affinity to CCR2 in human monocytes
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
72947411 105255 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115272 105255 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11721085 166857 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL428559 166857 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 565 13 2 5 7.4 CCN(CC)CCCC(C)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
56671792 65792 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834787 65792 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 3 5 3.9 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.08.074
11640044 148245 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 405 5 1 1 6.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393631 148245 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 405 5 1 1 6.2 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCCC1 10.1016/j.bmcl.2007.01.115
44425308 153704 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL398150 153704 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44573486 193156 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523054 193156 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOCC2)C1 10.1016/j.bmcl.2008.12.050
90656025 111118 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 483 4 0 6 2.7 COC1COCCC1N(C)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263280 111118 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 483 4 0 6 2.7 COC1COCCC1N(C)[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
76335990 105237 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115113 105237 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44453535 155172 None 1 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL402322 155172 None 1 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 473 6 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
25033361 154481 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cell membraneDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cell membrane
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399045 154481 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cell membraneDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cell membrane
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
25033361 154481 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399045 154481 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 490 5 0 2 6.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44353367 117301 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 344 3 1 3 4.6 N#Cc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL339670 117301 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 344 3 1 3 4.6 N#Cc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
44442542 93763 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 10 4 4 2.2 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247406 93763 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 464 10 4 4 2.2 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
10409097 66640 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 406 5 2 5 2.4 O=C(CN1CCCN(Cc2ccc(Cl)cc2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
CHEMBL185282 66640 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 406 5 2 5 2.4 O=C(CN1CCCN(Cc2ccc(Cl)cc2)CC1)NNC(=O)c1cccs1 10.1016/j.bmcl.2004.08.008
127027624 137386 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cc(C)cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3753178 137386 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cc(C)cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
10277182 98000 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 2 3 4.6 Cc1ccc(CN(C)[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272860 98000 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 7 2 3 4.6 Cc1ccc(CN(C)[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
22394337 117088 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
CHEMBL339275 117088 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1cccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)c1 10.1016/j.bmcl.2003.10.049
24801690 98039 None 25 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to CCR2 T292A mutantBinding affinity to CCR2 T292A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98039 None 25 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to CCR2 T292A mutantBinding affinity to CCR2 T292A mutant
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
46830336 7848 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7848 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
11214277 74535 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccnc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029415 74535 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccnc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1021/ml200199c
44453268 95127 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 462 7 3 4 2.8 CC(=O)Nc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL255585 95127 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 462 7 3 4 2.8 CC(=O)Nc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
89823413 126331 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
CHEMBL3650381 126331 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
44453474 97869 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272284 97869 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 512 6 3 4 2.6 Nc1ccc(I)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
72946198 105232 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115108 105232 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10299408 73698 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018363 73698 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46946058 65430 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 504 7 2 6 2.8 CN(C)c1ncc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829623 65430 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 504 7 2 6 2.8 CN(C)c1ncc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
56683121 65809 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834853 65809 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
56676474 65810 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834854 65810 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 6 2 7 4.2 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3nccs3)CC2)C1 10.1016/j.bmcl.2011.08.074
53322811 58472 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683077 58472 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54583112 62544 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782378 62544 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 513 6 0 7 3.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
46240380 83561 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 519 7 3 6 2.5 CN(C)c1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204245 83561 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 519 7 3 6 2.5 CN(C)c1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
57393531 70509 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946834 70509 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44442596 93470 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 593 11 5 6 3.8 CCOC(=O)Nc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246098 93470 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 593 11 5 6 3.8 CCOC(=O)Nc1cc(C(=O)NCC(=O)N[C@@H](CNCc2ccc(C)cc2C)C(=O)NC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
73351183 93232 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2448120 93232 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
44453477 155301 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL402988 155301 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
44443989 94446 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 414 8 1 2 5.3 O=C(/C=C/c1ccc(F)cc1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251217 94446 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 414 8 1 2 5.3 O=C(/C=C/c1ccc(F)cc1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
46886507 8082 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 594 9 4 6 5.7 CSc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1091266 8082 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 594 9 4 6 5.7 CSc1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
89823576 126327 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
CHEMBL3650377 126327 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
46842233 7716 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088875 7716 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
508741 167467 None 1 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
CHEMBL429912 167467 None 1 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 435 7 2 4 2.8 COc1cccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)c1 10.1016/j.bmcl.2008.02.015
90656017 111105 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 2 6 1.9 COC1COCCC1N[C@@H]1C[C@H]2NCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263264 111105 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 468 4 2 6 1.9 COC1COCCC1N[C@@H]1C[C@H]2NCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
72946198 105232 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115108 105232 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 624 7 1 8 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946199 105231 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115107 105231 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656854 75226 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036781 75226 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 425 3 2 4 2.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C(=O)[C@H]2CN(C3CC3)CCN2)CC1 10.1016/j.bmcl.2012.04.118
46944854 65427 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829620 65427 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1cnccc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
54754724 65752 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834645 65752 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 479 9 2 6 3.6 C=CCOC[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44425649 86127 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86127 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44413214 77798 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 421 4 1 5 4.9 Cc1ccc2c(c1)C1(CCN(CCc3coc(-c4ccc(F)cc4)n3)CC1)OC(=O)N2 10.1016/j.bmcl.2006.04.045
CHEMBL209263 77798 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 421 4 1 5 4.9 Cc1ccc2c(c1)C1(CCN(CCc3coc(-c4ccc(F)cc4)n3)CC1)OC(=O)N2 10.1016/j.bmcl.2006.04.045
53320349 58667 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 417 5 1 4 2.6 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684690 58667 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 417 5 1 4 2.6 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44570717 183830 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL480620 183830 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.2 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.12.062
44425256 86051 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 631 9 2 6 5.9 CC(=O)Nc1nc(C(CCN2CCN(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230791 86051 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 631 9 2 6 5.9 CC(=O)Nc1nc(C(CCN2CCN(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
89823552 126301 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650351 126301 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
76335990 105237 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115113 105237 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 4 1 6 2.1 COC1COCCC1N[C@@H]1C[C@H]2CN(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57344229 130639 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681887 130639 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 3 6.5 O=C(O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
10137967 153946 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL398354 153946 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2012.03.007
10137967 153946 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398354 153946 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 437 9 4 4 2.3 Cc1ccc(CNC[C@@H](CO)NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1016/j.bmcl.2007.07.028
44444099 154406 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL398844 154406 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844329 80038 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 592 7 1 2 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(CCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL212928 80038 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 592 7 1 2 7.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(CCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
23656584 89919 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 7 2 3 6.0 O=C(O)C(C1CCN(C(=O)CCc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237966 89919 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 541 7 2 3 6.0 O=C(O)C(C1CCN(C(=O)CCc2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44453327 95093 None 25 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL255408 95093 None 25 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2010.02.072
42632840 168709 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 364 5 1 3 3.6 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C#N)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL436822 168709 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 364 5 1 3 3.6 C[N+](C)(Cc1ccc(NC(=O)c2cccc(C#N)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
127025730 137320 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
CHEMBL3752640 137320 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
89823462 126356 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
CHEMBL3650404 126356 None 0 Human Binding pIC50 = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
72947411 105255 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115272 105255 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 598 6 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946381 105234 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115110 105234 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 609 7 1 8 2.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
69285563 121226 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577936 121226 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
67774071 130654 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681901 130654 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 521 7 3 4 4.3 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
54754844 65744 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 434 5 2 6 2.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C#N)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834638 65744 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 434 5 2 6 2.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C#N)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
71768831 111113 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 5 1 8 1.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263273 111113 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 499 5 1 8 1.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)C1 10.1016/j.bmcl.2014.03.036
122181238 121851 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589952 121851 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
23655673 146653 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL392366 146653 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
71518405 86398 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 5 1 3 4.7 CCC(CC)N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314055 86398 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 423 5 1 3 4.7 CCC(CC)N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
23655673 146653 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL392366 146653 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 1 4 5.3 COC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44395169 66155 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CNC2CCN(CCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL184240 66155 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 476 9 3 5 3.7 Cc1csc(C(=O)NNC(=O)CNC2CCN(CCC(c3ccccc3)c3ccccc3)C2)c1 10.1016/j.bmcl.2004.08.009
11690536 121220 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 431 12 4 4 2.7 CCC[C@H](O)[C@H](CNCCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577930 121220 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 431 12 4 4 2.7 CCC[C@H](O)[C@H](CNCCC(C)C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
71519224 86397 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 466 4 1 4 3.9 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314054 86397 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 466 4 1 4 3.9 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57400331 70524 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 551 9 3 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](NC2CCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1947044 70524 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 551 9 3 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](NC2CCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
57403811 70339 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 651 10 3 6 4.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944779 70339 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 651 10 3 6 4.1 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
53326703 58477 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 CCOC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683082 58477 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 514 8 1 7 2.7 CCOC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
89823551 126310 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
CHEMBL3650360 126310 None 0 Human Binding pIC50 = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
11215504 73800 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)OC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018527 73800 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 5.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)OC(C)(C)C)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57398590 70335 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 565 8 2 5 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](N2CCCCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1944775 70335 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 565 8 2 5 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CC[C@@H](N2CCCCC2)[C@@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
71768862 111115 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2ccnc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263275 111115 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2ccnc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
22310924 20166 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cccc(Cl)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130467 20166 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2cccc(Cl)c2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
22311000 20344 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2ccc(Cl)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130608 20344 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 353 3 1 2 5.3 O=C(O)c1cc2ccc(Cl)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44444006 94036 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 446 9 1 3 4.9 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248829 94036 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 446 9 1 3 4.9 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
23656432 154399 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 549 6 1 5 5.2 CC(=O)n1cc(C2CCN(C(C(=O)O)C3CCN(C(=O)/C=C/c4cc(F)cc(F)c4)CC3)CC2)c2ccccc21 10.1021/jm070902b
CHEMBL398796 154399 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 549 6 1 5 5.2 CC(=O)n1cc(C2CCN(C(C(=O)O)C3CCN(C(=O)/C=C/c4cc(F)cc(F)c4)CC3)CC2)c2ccccc21 10.1021/jm070902b
44395137 66191 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(F)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184390 66191 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(F)c3)c3cccc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
127028587 137554 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2ccc(Cl)cc2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3754549 137554 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 250 2 1 1 3.8 C[C@@]1(c2ccc(Cl)cc2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
44413328 139256 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378995 139256 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 487 8 2 3 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
25270182 93322 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 429 6 1 2 5.7 Cc1ccc(-c2cccc(C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)c2)cc1 10.1016/j.bmcl.2007.01.115
CHEMBL245290 93322 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 429 6 1 2 5.7 Cc1ccc(-c2cccc(C(=O)Nc3ccc(C[N+](C)(C)C4CCOCC4)cc3)c2)cc1 10.1016/j.bmcl.2007.01.115
46885159 8373 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1093153 8373 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
127027626 137248 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 266 2 1 1 3.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3751926 137248 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 266 2 1 1 3.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2015.11.051
44416015 81131 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215689 81131 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
72947193 105229 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115105 105229 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 568 6 1 7 3.3 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656749 75208 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036761 75208 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 444 4 1 3 4.4 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
49763571 65416 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829609 65416 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 459 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
70687885 74527 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029407 74527 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
71768931 111123 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 544 4 1 5 4.9 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263285 111123 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 544 4 1 5 4.9 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4COc5ccc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
44573487 192632 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1007/s00044-010-9501-4
CHEMBL521697 192632 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 496 6 2 3 6.0 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSCC2)C1 10.1007/s00044-010-9501-4
10141379 73701 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018366 73701 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 11 4 4 3.7 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
44425642 142344 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL388675 142344 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 582 5 1 3 7.3 CS[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
46885029 8247 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1092343 8247 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
71518571 86403 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 3 1 5 3.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCS(=O)(=O)CC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314060 86403 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 485 3 1 5 3.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCS(=O)(=O)CC1)C2 10.1016/j.bmcl.2012.10.069
71552097 86587 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315929 86587 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 7 3.6 Nc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
46240895 83576 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1021/ml300260s
CHEMBL2204260 83576 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3ccns3)CC2)C1 10.1021/ml300260s
46927116 65435 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829628 65435 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 4 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](O)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755919 65757 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834651 65757 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 6 2 7 4.5 O=C(CNc1noc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
44612590 137468 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753813 137468 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
53326702 58466 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683071 58466 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44425283 86059 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 648 10 2 6 6.2 CS(=O)(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230824 86059 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 648 10 2 6 6.2 CS(=O)(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425322 153199 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL397717 153199 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 738 9 2 5 8.6 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)C3Cc4ccccc43)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
44573488 187677 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495165 187677 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 482 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCSC2)C1 10.1016/j.bmcl.2008.12.050
44442577 93544 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.5 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246407 93544 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.5 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442578 155127 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 4 5 3.0 Cc1cc(N(C)C)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL402056 155127 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 535 10 4 5 3.0 Cc1cc(N(C)C)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
16720313 85415 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
CHEMBL226376 85415 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
53320967 58665 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 433 5 1 4 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684684 58665 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 433 5 1 4 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
24801344 97729 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 8 3 3 4.8 CC(C)c1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL271537 97729 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 8 3 3 4.8 CC(C)c1ccc(CN[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
44573410 187424 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493779 187424 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
44573410 187424 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493779 187424 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 7 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NCC2CCOCC2)C1 10.1007/s00044-010-9501-4
122181153 121838 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589847 121838 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
122181151 121837 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589846 121837 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 622 7 1 3 7.6 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
72946387 105224 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115100 105224 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 535 4 2 7 1.3 COC1COCCC1N[C@@H]1C[C@H]2CN(/C(N)=N\C#N)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11553070 75198 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036751 75198 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
46208367 83579 None 13 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83579 None 13 Human Binding pIC50 = 7.4 7.4 - 1
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
10195882 70504 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1946829 70504 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44415973 81053 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215394 81053 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 8 1 2 7.0 C=CC[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44415939 140131 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL380190 140131 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44442598 154385 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398747 154385 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 465 9 5 5 1.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2N)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
24801522 161135 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 161135 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
89823526 126345 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650394 126345 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
57344319 130633 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(F)c2)CC1 nan
CHEMBL3681881 130633 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cccc(F)c2)CC1 nan
9889422 127152 None 3 Human Binding pIC50 = 6.4 6.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL365681 127152 None 3 Human Binding pIC50 = 6.4 6.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
54755193 65743 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 437 6 3 4 4.0 CC(C)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834637 65743 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 437 6 3 4 4.0 CC(C)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57395061 70334 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 10 2 5 3.9 CCCN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944774 70334 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 10 2 5 3.9 CCCN(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
71768897 111121 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
CHEMBL3263283 111121 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 543 4 1 5 4.5 O=C(O)c1cccc(C2CCN([C@@H]3C[C@H]4OCC[C@@]4(C(=O)N4CCc5ncc(C(F)(F)F)cc5C4)C3)CC2)c1 10.1016/j.bmcl.2014.03.036
44353197 20768 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 450 4 1 4 4.6 O=C(NS(=O)(=O)C(F)(F)F)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130947 20768 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 450 4 1 4 4.6 O=C(NS(=O)(=O)C(F)(F)F)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
127025729 137322 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1C 10.1016/j.bmcl.2015.11.051
CHEMBL3752652 137322 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1C 10.1016/j.bmcl.2015.11.051
127036934 137426 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753474 137426 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 248 2 1 1 3.5 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cccc(F)c2)C1 10.1016/j.bmcl.2015.11.051
57391797 70508 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946833 70508 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
68004016 86606 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nccc2ncc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2316211 86606 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1nccc2ncc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
11342351 77639 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 592 10 2 5 5.5 CCCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088381 77639 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 592 10 2 5 5.5 CCCc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
44415898 81119 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215654 81119 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
53320970 58679 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 435 5 1 4 2.5 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684704 58679 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 435 5 1 4 2.5 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44442566 154776 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL400159 154776 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
22143196 183985 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183985 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44444005 93996 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 3 4.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248640 93996 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 428 9 1 3 4.8 COc1ccc(C2CCN(CCCCNC(=O)/C=C/c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2007.07.065
132572938 156787 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4070869 156787 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
44353377 23168 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL133111 23168 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 397 4 1 4 4.1 CS(=O)(=O)c1cccc2c1cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71552260 86596 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 574 6 3 8 4.2 O=C(CNc1nc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315938 86596 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 574 6 3 8 4.2 O=C(CNc1nc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
72946013 105257 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115274 105257 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
76333441 84897 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](NCCN1CCCCC1)c1ccsc1 10.1007/s00044-010-9497-9
CHEMBL2236473 84897 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](NCCN1CCCCC1)c1ccsc1 10.1007/s00044-010-9497-9
10323427 79758 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL211775 79758 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 493 8 2 4 5.2 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccsc1 10.1016/j.bmcl.2006.04.045
508877 95059 None 1 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL255209 95059 None 1 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
53321503 58490 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683188 58490 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 516 8 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CCCF)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
53321615 58678 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 451 5 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684703 58678 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 451 5 1 4 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)CC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
67772859 124445 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 535 7 2 4 5.6 COC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3639807 124445 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 535 7 2 4 5.6 COC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
10139782 73697 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018362 73697 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
49763569 65417 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 435 6 2 5 2.7 O=C(CNC(=O)c1ccccc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829610 65417 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 435 6 2 5 2.7 O=C(CNC(=O)c1ccccc1)NC1CN([C@H]2CC[C@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
25268436 93427 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(F)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245896 93427 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 2 4.5 C[N+](C)(Cc1ccc(NC(=O)c2ccc(F)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
9885442 20751 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cc([N+](=O)[O-])ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130936 20751 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 364 4 1 4 4.6 O=C(O)c1cc2cc([N+](=O)[O-])ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
89823586 126322 None 0 Human Binding pIC50 = 6.4 6.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
CHEMBL3650372 126322 None 0 Human Binding pIC50 = 6.4 6.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
72947413 105254 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115271 105254 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 510 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
162666730 182272 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Antagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay basedAntagonist activity at human CCR2 expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment pre-incubated for 20 mins before CCL2 stimulation and followed by further incubation for 90 mins by NanoBiT CCR2 assay based
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155491018 174081 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Antagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assayAntagonist activity at human TEV cleavage site-linked CCR2b expressed in human U2OS cells harboring beta-lactamase reporter gene assessed as inhibition of CCL2-induced beta-arrestin recruitment incubated for 30 mins followed by CCL2 stimulation and measured after 16 hrs by Tango assay
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
86767123 129404 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 497 5 1 6 3.1 CCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
CHEMBL3671256 129404 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 497 5 1 6 3.1 CCC1CC2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)CC(NC3CCOCC3OC)CC2O1 nan
11699149 95104 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255478 95104 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 511 6 2 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
10304021 73718 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018384 73718 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
44415880 169337 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL441856 169337 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44447775 95705 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL258246 95705 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 1 2 7.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425643 86040 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230722 86040 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425271 153240 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 598 10 2 5 6.4 O=CNc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397747 153240 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 598 10 2 5 6.4 O=CNc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44593562 187493 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187493 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
71768755 111098 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 5 1 6 3.1 CCC1C[C@@]2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)C[C@H](NC3CCOCC3OC)C[C@H]2O1 10.1016/j.bmcl.2014.03.036
CHEMBL3263256 111098 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 5 1 6 3.1 CCC1C[C@@]2(C(=O)N3CCc4ncc(C(F)(F)F)cc4C3)C[C@H](NC3CCOCC3OC)C[C@H]2O1 10.1016/j.bmcl.2014.03.036
11591956 89335 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 6.1 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236930 89335 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 6.1 O=C(O)C(C1CCN(C(=O)/C=C/c2ccc(Cl)c(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656430 89879 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 540 6 3 4 4.8 Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL237806 89879 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 540 6 3 4 4.8 Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
11548199 89920 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237967 89920 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)[C@H](C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
23656431 146335 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.5 Cc1[nH]c2ccccc2c1C1CCN(C(C(=O)O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1021/jm070902b
CHEMBL392120 146335 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 539 6 2 3 5.5 Cc1[nH]c2ccccc2c1C1CCN(C(C(=O)O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1021/jm070902b
44453405 95434 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
CHEMBL257062 95434 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
53318316 58677 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 453 4 1 5 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684702 58677 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 453 4 1 5 3.1 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57395219 71009 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
CHEMBL1951770 71009 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncc3)CC2)C1 10.1021/ml200030q
53320973 58688 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 453 6 1 5 3.0 CC(C)COC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684713 58688 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 453 6 1 5 3.0 CC(C)COC(=O)N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]1(C(C)C)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
44580590 193569 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 193569 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
24794585 179522 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4741305 179522 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Antagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assayAntagonist activity at CCR2 in human THP1 cells assessed as reduction in MCP1-induced chemotaxis measured after 30 mins by calcein-AM dye based fluorescence assay
ChEMBL 478 5 2 6 2.6 CC(=O)N[C@@H]1C[C@H](N(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
11283842 73736 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018402 73736 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11273379 74546 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029567 74546 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
54583111 62543 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782377 62543 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 512 6 0 6 3.7 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
24794583 181091 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
CHEMBL4760098 181091 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 464 5 3 6 2.3 CN[C@@H]1CC[C@H](N2CC[C@H](Nc3ncnc4ccc(C(F)(F)F)cc34)C2=O)[C@H](NC(C)=O)C1 10.1021/acsmedchemlett.1c00082
53321616 58458 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683063 58458 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
25110716 155204 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
CHEMBL402532 155204 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in human monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in human monocytes
ChEMBL 515 4 0 3 7.0 C[C@H]1CN([C@@H]2CC[C@@]3(CCO[C@H]3OCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.016
44573485 187719 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495368 187719 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2008.12.050
44573452 187605 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1007/s00044-010-9501-4
CHEMBL494770 187605 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1007/s00044-010-9501-4
68764898 671 None 2 Human Binding pIC50 = 8.3 8.3 - 3
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
9430 671 None 2 Human Binding pIC50 = 8.3 8.3 - 3
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
CHEMBL3577945 671 None 2 Human Binding pIC50 = 8.3 8.3 - 3
Antagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulationAntagonist activity against CCR2 in whole blood (unknown origin) assessed as reduction in CD11b upregulation
ChEMBL 491 7 1 5 5.3 CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/ml500505q
10281715 73721 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018387 73721 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
10281715 73721 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL2018387 73721 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
69286635 121229 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577939 121229 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 469 9 2 3 4.9 CC(C)CC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
44571218 183876 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183876 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57398750 71014 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
CHEMBL1951775 71014 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccnnc3)CC2)C1 10.1021/ml200030q
66768640 121224 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL3577934 121224 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 515 13 6 5 2.6 CCC[C@H](O)[C@H](CNCC1CC1)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
68004002 86582 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315924 86582 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 506 6 3 8 3.1 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
67774784 130648 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681896 130648 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
11712754 95064 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 482 5 3 3 4.9 O=C(Nc1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255266 95064 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 482 5 3 3 4.9 O=C(Nc1cc(F)cc(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11555541 155293 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 529 6 2 3 5.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL402955 155293 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 529 6 2 3 5.2 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11192300 73801 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018528 73801 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 565 13 6 5 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC(=O)NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11718088 93580 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 1 5.8 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCC1 10.1016/j.bmcl.2007.01.115
CHEMBL246520 93580 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 391 5 1 1 5.8 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCCC1 10.1016/j.bmcl.2007.01.115
71519054 86395 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 432 4 1 4 3.6 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314052 86395 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 432 4 1 4 3.6 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(Cl)cc3C2)C1 10.1016/j.bmcl.2012.10.069
10436083 79875 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL212306 79875 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44442565 93539 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246401 93539 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
10299952 155009 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 488 10 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL401463 155009 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 488 10 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
24801343 97771 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(C(F)(F)F)cc1 10.1021/jm701488f
CHEMBL271752 97771 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(C(F)(F)F)cc1 10.1021/jm701488f
44395165 169471 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 2 6 3.4 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(CO)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL442966 169471 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 2 6 3.4 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(CO)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44444098 161662 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1cccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2007.07.065
CHEMBL413084 161662 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 6 0 3 6.1 COc1cccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)c1 10.1016/j.bmcl.2007.07.065
44395129 66642 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 8 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL185283 66642 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 8 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
57344313 130655 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL3681902 130655 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
57344303 130647 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681895 130647 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
71517239 86372 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@H]1C[C@@H]2CCC[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313766 86372 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@H]1C[C@@H]2CCC[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
72946200 105230 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115106 105230 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72946008 105235 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115111 105235 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
53321483 58473 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683078 58473 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 7 1 6 3.5 CCC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
10279078 73713 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 11 5 5 3.5 CCC(O)(CC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018379 73713 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 11 5 5 3.5 CCC(O)(CC)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46240687 83583 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204267 83583 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 528 7 3 7 3.2 CSc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44447786 95112 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255511 95112 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
54584109 62545 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782379 62545 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 509 5 1 6 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
69286108 121231 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577941 121231 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
10218812 193432 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 621 10 3 7 2.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NS(C)(=O)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526180 193432 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 621 10 3 7 2.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NS(C)(=O)=O)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
89823580 126335 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
CHEMBL3650385 126335 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
57344314 68928 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922788 68928 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
76314234 105221 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115098 105221 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
72945830 105225 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115101 105225 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
49764701 65437 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 500 6 3 5 2.9 N#Cc1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
CHEMBL1829630 65437 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 500 6 3 5 2.9 N#Cc1cccc([C@]2(O)CC[C@@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2011.06.080
44442543 154819 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 11 4 4 2.9 CCNC(=O)[C@H](CCNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400383 154819 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 11 4 4 2.9 CCNC(=O)[C@H](CCNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
22310945 118059 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL340450 118059 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395186 65216 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 478 8 1 5 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL182598 65216 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 478 8 1 5 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
57397013 70511 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 343 4 3 3 1.8 N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1946836 70511 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 343 4 3 3 1.8 N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44395143 67012 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CNC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186984 67012 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CNC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
24801345 97852 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97852 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
24801345 97852 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97852 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
122181152 121704 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3588870 121704 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
5353432 97493 None 89 Human Binding pIC50 = 5.4 5.4 -1 3
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97493 None 89 Human Binding pIC50 = 5.4 5.4 -1 3
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
44573569 193287 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1007/s00044-010-9501-4
CHEMBL524030 193287 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1007/s00044-010-9501-4
44573569 193287 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
CHEMBL524030 193287 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 3 6.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
44415904 80428 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214641 80428 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 514 9 1 2 7.0 CCC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44425306 142367 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388949 142367 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44453408 95436 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257064 95436 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 436 6 4 5 2.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(O)cc2)C1 10.1016/j.bmcl.2008.02.015
44593562 187493 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187493 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
49863225 15213 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 609 13 5 7 4.4 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL1210728 15213 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 609 13 5 7 4.4 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44395136 67077 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 493 8 2 6 3.5 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(N)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187284 67077 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 493 8 2 6 3.5 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(N)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
9842404 67272 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 371 6 2 3 2.5 O=C(CNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL188170 67272 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 371 6 2 3 2.5 O=C(CNC(=O)c1ccccc1)NC1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44413147 139711 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2006.04.045
CHEMBL379818 139711 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccsc1 10.1016/j.bmcl.2006.04.045
25269516 93321 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 353 5 1 2 4.0 Cc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
CHEMBL245289 93321 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 353 5 1 2 4.0 Cc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
44439166 90544 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238731 90544 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 595 12 5 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCNc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11237256 73732 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018398 73732 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46945254 65433 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829626 65433 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1cccnc1[C@H]1CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
89823575 126309 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
CHEMBL3650359 126309 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
89823628 126347 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650396 126347 None 0 Human Binding pIC50 = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
11585168 90686 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239143 90686 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44442573 93541 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 10 4 5 2.7 CN(C)c1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246404 93541 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 521 10 4 5 2.7 CN(C)c1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
44395125 123116 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 409 7 0 3 5.3 N#Cc1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL361121 123116 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 409 7 0 3 5.3 N#Cc1ccc(CN2CCCN(CCC(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
508727 155317 None 1 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 389 6 2 3 2.6 O=C(CNC(=O)c1cccc(F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL403058 155317 None 1 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 389 6 2 3 2.6 O=C(CNC(=O)c1cccc(F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44415945 139547 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CC[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL379634 139547 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CC[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
127028592 137498 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.4 C[C@@]1(c2ccc(Cl)c(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
CHEMBL3754037 137498 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 284 2 1 1 4.4 C[C@@]1(c2ccc(Cl)c(Cl)c2)CCCC=C1C(=O)O 10.1016/j.bmcl.2015.11.051
11585168 90686 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239143 90686 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46241509 83560 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204244 83560 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46945857 65429 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 461 6 2 5 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cnccn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829622 65429 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 461 6 2 5 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cnccn3)CC2)C1 10.1016/j.bmcl.2011.06.080
54754722 65750 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834643 65750 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 439 6 3 6 2.4 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](CO)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
10030247 95406 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256954 95406 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccncn3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425634 142016 None 0 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL387587 142016 None 0 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10240278 172895 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451597 172895 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 654 10 4 6 5.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
69321774 73808 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 593 13 5 5 4.4 CCC[C@H](O)[C@H](CN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018536 73808 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 593 13 5 5 4.4 CCC[C@H](O)[C@H](CN(C)Cc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1016/j.bmcl.2012.03.007
11844471 80197 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CCC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL213648 80197 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 618 8 1 2 8.4 CCC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
71519053 86394 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 4 1 4 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314051 86394 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 4 1 4 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ccc(F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11570045 90947 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239358 90947 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11570045 90947 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239358 90947 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 530 13 1 4 7.3 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2ccc(Cl)cc2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46885028 8420 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1093470 8420 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
89823601 126358 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650406 126358 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
70696470 75216 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
CHEMBL2036769 75216 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 367 4 1 4 2.6 N#Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1 10.1016/j.bmcl.2012.04.118
72946775 105233 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115109 105233 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 597 7 2 8 1.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCNC(C)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71517401 86379 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313773 86379 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 501 4 1 5 3.5 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](Cl)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
51039119 176215 None 33 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-CCL2 from mouse CCR2Displacement of [125I]-CCL2 from mouse CCR2
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176215 None 33 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-CCL2 from mouse CCR2Displacement of [125I]-CCL2 from mouse CCR2
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
46241826 83559 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204243 83559 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 490 6 3 5 2.8 Cc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
56667036 65425 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829618 65425 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 460 6 2 4 3.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44447789 155220 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 600 7 3 4 6.2 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL402624 155220 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 600 7 3 4 6.2 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
44453472 155536 None 1 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2b in HEK293 cellsDisplacement of [125I]MCP1 from human CCR2b in HEK293 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404259 155536 None 1 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from human CCR2b in HEK293 cellsDisplacement of [125I]MCP1 from human CCR2b in HEK293 cells
ChEMBL 454 6 3 4 3.1 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44425640 96927 None 0 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL266017 96927 None 0 Mouse Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
11844470 141734 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL385824 141734 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCC12C=Cc1ccccc12 10.1021/jm060439n
11456448 77643 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 640 10 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Cc3ccccc3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088385 77643 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 640 10 2 5 6.2 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(Cc3ccccc3)cc2)C1 10.1016/j.bmcl.2012.08.002
53321427 58464 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683069 58464 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
89823598 126363 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650410 126363 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44395094 67255 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(Cl)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL188075 67255 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 528 8 2 6 4.3 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cccc(Cl)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
46886057 8397 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1093319 8397 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
44612589 137430 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753491 137430 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44444000 94509 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1cc(Cl)cc(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL251620 94509 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 464 8 1 2 6.4 O=C(/C=C/c1cc(Cl)cc(Cl)c1)NCCCCN1CCC(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.07.065
44395254 66240 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 564 10 1 7 4.1 CN(C)c1ccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccc(N(C)C)cc2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL184582 66240 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 564 10 1 7 4.1 CN(C)c1ccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccc(N(C)C)cc2)cc1 10.1016/j.bmcl.2004.08.008
10153431 188327 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 643 9 3 7 5.7 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL500786 188327 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 643 9 3 7 5.7 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2009.05.041
11641253 58451 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 464 5 1 3 5.3 CC(C)[C@]1(C(=O)N2CC=C(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683054 58451 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 464 5 1 3 5.3 CC(C)[C@]1(C(=O)N2CC=C(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
53324140 58460 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683065 58460 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
89823656 126353 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650401 126353 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
53318854 58467 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683072 58467 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.2 COC[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
9852285 8258 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 634 7 3 6 5.8 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092434 8258 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 634 7 3 6 5.8 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2N2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3NC(=O)OC(C)(C)C)C2=O)cc1 10.1016/j.bmcl.2010.03.035
44415942 138679 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 534 8 2 3 5.7 CC(O)C(CCN1CCC(c2ccc(F)cc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL377819 138679 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 534 8 2 3 5.7 CC(O)C(CCN1CCC(c2ccc(F)cc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
53326700 58461 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683066 58461 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 495 6 1 4 5.0 CC[C@@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
22143314 193200 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 522 8 3 5 3.1 CSc1ccc(CNC2CCN(C(C)=O)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL523403 193200 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 522 8 3 5 3.1 CSc1ccc(CNC2CCN(C(C)=O)CC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
122181236 121849 None 0 Mouse Binding pIC50 = 5.3 5.3 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589950 121849 None 0 Mouse Binding pIC50 = 5.3 5.3 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 588 8 1 4 6.3 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
44593561 12661 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
CHEMBL1187238 12661 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
CHEMBL494580 12661 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1007/s00044-010-9501-4
44593561 12661 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12661 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12661 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
44415992 80607 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215093 80607 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
52950180 19348 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290754 19348 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
44442576 93543 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 2.9 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246406 93543 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 522 10 4 5 2.9 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44423285 142164 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 7.0 C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
CHEMBL388380 142164 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 536 4 1 2 7.0 C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
89823445 126349 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650398 126349 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
57344295 130623 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681872 130623 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
23656067 148985 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL394228 148985 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
23656067 148985 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1021/jm070902b
CHEMBL394228 148985 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 481 5 1 2 5.7 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1021/jm070902b
86698131 126304 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
CHEMBL3650354 126304 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 582 5 1 5 5.4 O=C(O)c1cccc(C2CCN([C@H]3C[C@H]4CCC[C@@]4(C(=O)N4C[C@@H]5C[C@H]4CN5c4cc(C(F)(F)F)ccn4)C3)CC2)c1 nan
44439160 169395 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL442254 169395 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44439160 169395 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL442254 169395 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 11 4 6 4.9 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
25267738 93868 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 339 5 1 2 3.7 C[N+](C)(Cc1ccc(NC(=O)c2ccccc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL247949 93868 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 339 5 1 2 3.7 C[N+](C)(Cc1ccc(NC(=O)c2ccccc2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
22311005 19980 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 458 5 1 4 5.1 O=C(NS(=O)(=O)c1ccccc1)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130318 19980 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 458 5 1 4 5.1 O=C(NS(=O)(=O)c1ccccc1)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44415864 80544 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 554 7 2 3 6.0 CC(O)C(CCN1CC[C@@]2(C=Cc3ccccc32)[C@@H](C)C1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL214825 80544 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 554 7 2 3 6.0 CC(O)C(CCN1CC[C@@]2(C=Cc3ccccc32)[C@@H](C)C1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
10164316 154790 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL400196 154790 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 9 4 4 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
56683120 65805 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 476 6 2 7 3.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ncco4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834849 65805 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 476 6 2 7 3.5 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ncco4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44449229 95146 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 538 7 1 3 5.6 CN(C)CC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL255687 95146 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 538 7 1 3 5.6 CN(C)CC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
44453134 98062 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL273195 98062 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 455 7 2 4 3.4 O=C(CNC(=O)c1cccc(OC(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
11155781 73807 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 476 10 4 4 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)Cc1nc2c(C(F)(F)F)cccc2[nH]1 10.1016/j.bmcl.2012.03.007
CHEMBL2018534 73807 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 476 10 4 4 4.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)Cc1nc2c(C(F)(F)F)cccc2[nH]1 10.1016/j.bmcl.2012.03.007
46241610 83568 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204252 83568 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
71519381 86371 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL2313765 86371 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
89823417 126343 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
CHEMBL3650392 126343 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
44442563 93732 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 9 3 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCOCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247211 93732 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 9 3 5 2.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)N2CCOCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344221 68955 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 nan
CHEMBL1922819 68955 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 568 8 3 4 5.5 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(OC(F)(F)F)cc2)CC1 nan
54772203 86589 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315931 86589 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cccnc3)CC2)C1 10.1016/j.bmcl.2012.12.017
54771980 86592 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccn3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315934 86592 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 484 6 2 6 4.0 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccn3)CC2)C1 10.1016/j.bmcl.2012.12.017
71190126 84899 None 1 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1007/s00044-010-9497-9
CHEMBL2236475 84899 None 1 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at Homo sapiens (human) CCR2 receptorAntagonist activity at Homo sapiens (human) CCR2 receptor
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1007/s00044-010-9497-9
56643545 130621 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681870 130621 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
57344303 130646 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130646 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
11591776 145484 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL391459 145484 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
11185 1989 None 42 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
25134303 1989 None 42 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
CHEMBL2178573 1989 None 42 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
DB16066 1989 None 42 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 495 5 2 6 4.4 Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2 10.1021/jm300682j
11598084 75202 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036755 75202 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 474 6 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
10162782 73704 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018370 73704 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
70691784 73705 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018371 73705 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 493 12 4 4 3.9 CCCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46241010 83582 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204266 83582 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 540 8 3 7 3.3 CC(C)Oc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
49763568 65413 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829605 65413 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
56657930 65791 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
CHEMBL1834786 65791 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 528 7 2 6 4.6 CN(C)c1cccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)c1 10.1016/j.bmcl.2011.08.074
56683116 65804 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834799 65804 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
89845031 109811 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 6 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
CHEMBL3233183 109811 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 533 8 1 6 2.8 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(OC(F)(F)F)c3)C2=O)[C@H](CS(C)(=O)=O)C1 10.1016/j.bmcl.2014.02.013
9850318 95243 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL256154 95243 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425646 86098 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231038 86098 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 528 6 1 2 7.1 CCCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53317027 58664 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 435 4 1 5 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684683 58664 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 435 4 1 5 3.2 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.052
44425645 86080 None 0 Mouse Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86080 None 0 Mouse Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10162782 73704 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL2018370 73704 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 479 11 4 4 3.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
11591776 145484 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL391459 145484 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 525 6 2 3 5.2 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
24801690 98039 None 25 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 98039 None 25 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
10008367 2020 None 50 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2020 None 50 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2020 None 50 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2020 None 50 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
24801690 98039 None 25 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98039 None 25 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
57656833 75227 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Inhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cellsInhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cells
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75227 None 0 Human Binding pIC50 = 8.3 8.3 - 1
Inhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cellsInhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cells
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
68767109 109810 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 7 1 5 3.3 Cc1ccc(C(=O)N[C@H]2CCN([C@H]3CC[C@@H](N(C)C(C)C)C[C@H]3CS(C)(=O)=O)C2=O)cc1C(F)(F)F 10.1016/j.bmcl.2014.02.013
CHEMBL3233182 109810 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMCDisplacement of [125I]-labeled human MCP1 from CCR2 in human PBMC
ChEMBL 531 7 1 5 3.3 Cc1ccc(C(=O)N[C@H]2CCN([C@H]3CC[C@@H](N(C)C(C)C)C[C@H]3CS(C)(=O)=O)C2=O)cc1C(F)(F)F 10.1016/j.bmcl.2014.02.013
57400451 70505 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
CHEMBL1946830 70505 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 9 3 5 3.6 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2011.12.057
44425249 143520 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL389888 143520 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11192346 2022 None 57 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2022 None 57 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2022 None 57 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
10165625 73726 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018392 73726 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 536 13 5 5 4.3 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)C 10.1016/j.bmcl.2012.03.007
44453365 97525 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL270435 97525 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 465 7 4 6 2.0 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
11227168 74548 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029569 74548 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 596 6 2 9 3.6 O=C(C1CCN(c2nccc(C(F)(F)F)n2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44573650 193208 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1007/s00044-010-9501-4
CHEMBL523503 193208 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1007/s00044-010-9501-4
44425648 168702 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL436796 168702 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 540 6 1 2 7.1 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573649 187233 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492569 187233 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
67011331 74543 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029424 74543 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 557 7 3 7 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncco4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44593563 193108 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193108 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
53324304 58462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11387511 74539 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029419 74539 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ccncc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10167417 73723 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018389 73723 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 591 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCCC1 10.1016/j.bmcl.2012.03.007
44583281 188233 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 188233 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
44425310 142356 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388868 142356 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 651 8 3 5 6.8 CNC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
11285792 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
801 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
CHEMBL2110727 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
DB11758 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR2 assessed as inhibition of CCL2 bindingAntagonist activity at CCR2 assessed as inhibition of CCL2 binding
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm300682j
11285792 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
801 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
CHEMBL2110727 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
DB11758 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from CCR2b expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
11285792 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
801 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
CHEMBL2110727 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
DB11758 878 None 34 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR2 (unknown origin)Inhibition of CCR2 (unknown origin)
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/acs.jmedchem.9b01701
44573649 187233 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1007/s00044-010-9501-4
CHEMBL492569 187233 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1007/s00044-010-9501-4
11534473 90697 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.ejmech.2010.04.024
CHEMBL239144 90697 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.ejmech.2010.04.024
71552261 86597 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 573 6 3 7 4.8 O=C(CNc1cc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315939 86597 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 573 6 3 7 4.8 O=C(CNc1cc(C(F)(F)F)nc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
11526729 155060 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL401744 155060 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2c(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c[nH]c2c1 10.1016/j.bmcl.2008.05.010
44448776 155254 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 572 6 3 5 5.7 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL402801 155254 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 572 6 3 5 5.7 COC(=O)c1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)Nc5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
57656825 75206 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036759 75206 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 394 4 1 3 3.5 O=C(Nc1ccc(F)c(Cl)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46241608 83567 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204251 83567 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 534 8 3 6 3.2 CC(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
46886482 8257 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 608 8 4 6 5.4 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1092433 8257 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human PBMC after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human PBMC after 30 mins
ChEMBL 608 8 4 6 5.4 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2010.03.035
10482463 95460 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnn3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL257160 95460 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnn3)CC2)C1 10.1016/j.bmcl.2007.12.029
183790 3740 None 11 Human Binding pIC50 = 7.3 7.3 -6 2
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3740 None 11 Human Binding pIC50 = 7.3 7.3 -6 2
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3740 None 11 Human Binding pIC50 = 7.3 7.3 -6 2
Displacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysisDisplacement of [3H]INCB3344 from human CCR2 expressed in human U2OS cells after 120 mins by scintillation spectrometric analysis
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
11671120 89878 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070902b
CHEMBL237805 89878 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 543 6 2 3 5.3 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070902b
22310995 20328 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130598 20328 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 334 3 2 3 4.3 Nc1ccc2c(c1)cc(C(=O)O)n2Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
17866152 124037 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 507 9 2 6 4.0 CNc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL363059 124037 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 507 9 2 6 4.0 CNc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
44395239 66151 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 412 9 1 3 4.7 O=C(CCCC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL184220 66151 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 412 9 1 3 4.7 O=C(CCCC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
46886056 8396 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 607 10 1 5 5.2 CCCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1093318 8396 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 607 10 1 5 5.2 CCCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
11466237 74536 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1cccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml200199c
CHEMBL2029416 74536 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1cccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml200199c
52944966 19038 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
CHEMBL1288324 19038 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 579 9 2 4 5.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1OCc1ccccc1 10.1016/j.bmcl.2010.10.020
44573609 187551 None 1 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494542 187551 None 1 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 496 6 3 4 4.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2O)C1 10.1016/j.bmcl.2008.12.050
44593564 187230 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1007/s00044-010-9501-4
CHEMBL492564 187230 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1007/s00044-010-9501-4
11296618 77642 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 632 9 2 6 6.3 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(-c3cccs3)cc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088384 77642 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 632 9 2 6 6.3 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccc(-c3cccs3)cc2)C1 10.1016/j.bmcl.2012.08.002
89823450 126344 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650393 126344 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
56678497 65716 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 2 4 4.5 O=C(COc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834581 65716 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 6 2 4 4.5 O=C(COc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
54754845 65749 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 452 6 3 6 1.8 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(N)=O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834642 65749 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 452 6 3 6 1.8 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(N)=O)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44444102 94033 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 5 1 3 5.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL248813 94033 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 5 1 3 5.8 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N1CCC(CN2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44425321 86134 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL231150 86134 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
11582651 75201 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036754 75201 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46944855 65432 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829625 65432 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccncc3O)CC2)C1 10.1016/j.bmcl.2011.06.080
44439170 151919 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 16 1 5 8.6 CCCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL396622 151919 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 16 1 5 8.6 CCCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44444107 154482 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 500 5 0 2 6.2 O=C(/C=C/c1ccc(Br)cc1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
CHEMBL399046 154482 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 500 5 0 2 6.2 O=C(/C=C/c1ccc(Br)cc1)N1CCC(CN2CCC(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmcl.2007.07.065
44413311 77781 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 473 8 2 3 4.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL209171 77781 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 473 8 2 3 4.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
89823456 124409 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
CHEMBL3639492 124409 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
11605985 90965 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239569 90965 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
11605985 90965 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239569 90965 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 514 13 1 4 6.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cccc(F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44416070 138891 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 623 8 4 4 4.0 O=C1NCC(C(=O)NC(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2006.07.011
CHEMBL378258 138891 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 623 8 4 4 4.0 O=C1NCC(C(=O)NC(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2006.07.011
89823427 126308 None 0 Human Binding pIC50 = 6.3 6.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
CHEMBL3650358 126308 None 0 Human Binding pIC50 = 6.3 6.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
11296325 77619 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3ccc(C(F)(F)F)cc3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
CHEMBL2088209 77619 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 596 9 2 6 5.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)Cc2nc3ccc(C(F)(F)F)cc3[nH]2)cc1 10.1016/j.bmcl.2012.08.002
71530223 86370 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313764 86370 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
53320171 58474 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683079 58474 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 512 7 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC(C)C)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
54756156 65783 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834779 65783 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 507 9 2 7 3.6 C=CCn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](C(=O)OCC)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44453325 155539 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
CHEMBL404269 155539 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 466 7 4 6 2.1 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1O 10.1016/j.bmcl.2008.02.015
56675300 65753 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 411 5 4 5 2.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834646 65753 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 411 5 4 5 2.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](O)CC2)C1 10.1016/j.bmcl.2011.08.074
44442572 93540 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246403 93540 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 506 10 4 4 3.2 CCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
24801342 97613 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 517 8 3 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(OC(F)(F)F)cc1 10.1021/jm701488f
CHEMBL270957 97613 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 517 8 3 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(OC(F)(F)F)cc1 10.1021/jm701488f
46240582 83571 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccnc1[C@]1(O)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1021/ml300260s
CHEMBL2204255 83571 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 479 6 3 6 1.8 Cn1ccnc1[C@]1(O)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1021/ml300260s
57403877 70523 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 10 3 5 3.6 CCCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1947043 70523 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 539 10 3 5 3.6 CCCN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44353447 3773 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
785 3773 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
CHEMBL337246 3773 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
52950180 19348 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290754 19348 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 545 10 2 4 5.1 CCCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
89823537 126296 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650346 126296 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
10115566 97409 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL269898 97409 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 7 3 3 4.3 Cc1ccc(CN[C@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
56681842 65714 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 5 2 4 3.9 O=C(Cn1[nH]c2ccc(C(F)(F)F)cc2c1=O)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834579 65714 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 472 5 2 4 3.9 O=C(Cn1[nH]c2ccc(C(F)(F)F)cc2c1=O)NC1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.08.074
127025159 137349 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 375 3 1 3 3.7 C[C@H]1CC=C(C(=O)NS(C)(=O)=O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752915 137349 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 375 3 1 3 3.7 C[C@H]1CC=C(C(=O)NS(C)(=O)=O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
56661444 65773 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834717 65773 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 614 6 3 8 5.1 CC(C)(C)NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
23405932 93730 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(F)(F)F)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247209 93730 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 532 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC(F)(F)F)c(C)c1 10.1016/j.bmcl.2007.07.028
89823506 126334 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650384 126334 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
44573485 187719 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1007/s00044-010-9501-4
CHEMBL495368 187719 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2)C1 10.1007/s00044-010-9501-4
127036603 137510 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc(C)c([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3754155 137510 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 258 2 1 1 4.0 Cc1ccc(C)c([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
24801346 161247 None 1 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 6 3 3 3.6 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL411935 161247 None 1 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 461 6 3 3 3.6 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
508749 67121 None 1 Human Binding pIC50 = 5.3 5.3 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 7 2 3 3.4 Cc1cccc(C(=O)NCC(=O)NCC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL187469 67121 None 1 Human Binding pIC50 = 5.3 5.3 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 7 2 3 3.4 Cc1cccc(C(=O)NCC(=O)NCC2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
57656701 75229 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 2 1 4 1.9 CN1CCN(C)C(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036784 75229 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 413 2 1 4 1.9 CN1CCN(C)C(C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10225909 93959 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 451 9 4 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248417 93959 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 451 9 4 4 2.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)O)c(C)c1 10.1016/j.bmcl.2007.07.028
57344222 130634 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1ccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 nan
CHEMBL3681882 130634 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1ccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 nan
44425649 86127 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86127 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
68004146 86586 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315928 86586 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 530 7 3 8 3.1 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4ncnc5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2012.12.017
54756045 65786 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834781 65786 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56671793 65794 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834789 65794 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44573452 187605 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494770 187605 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 480 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCOC2)C1 10.1016/j.bmcl.2008.12.050
10427222 165739 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cc(F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL424638 165739 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2cc(F)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
46886057 8397 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
CHEMBL1093319 8397 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 639 9 1 6 5.5 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2N2CCC(C)(NC(=O)c3cccc(C(F)(F)F)c3)C2=O)cc1 10.1016/j.bmcl.2010.03.035
72945827 105226 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115102 105226 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44442531 153943 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL398353 153943 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 478 10 4 4 2.5 CCNC(=O)[C@@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
71519052 86393 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 457 6 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(OC(C)C)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2314050 86393 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 457 6 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(OC(C)C)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44442584 93549 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 534 12 4 4 4.0 CCCCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246413 93549 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 534 12 4 4 4.0 CCCCc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
11590644 121221 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 11 4 4 3.3 CCC[C@H](O)[C@H](CNCC1CCCCC1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577931 121221 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 457 11 4 4 3.3 CCC[C@H](O)[C@H](CNCC1CCCCC1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
72948000 105222 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115099 105222 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 601 6 2 6 3.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46240585 83581 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204265 83581 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 524 7 3 6 3.6 CC(C)c1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
44425643 86040 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230722 86040 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 500 4 1 2 6.3 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
70697571 77973 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2096788 77973 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
57398651 70518 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 385 6 3 3 2.9 CC(C)N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1947039 70518 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 385 6 3 3 2.9 CC(C)N[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44416273 138939 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL378449 138939 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 496 6 1 2 6.2 O=C(CCCN1CCC2(C=Cc3ccccc32)CC1)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
90656015 111104 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 501 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2[S+]([O-])CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263262 111104 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 501 4 1 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2[S+]([O-])CC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
44413344 139336 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 489 8 2 4 4.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL379278 139336 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 489 8 2 4 4.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(NCCN1CCOCC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44353369 23241 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1 10.1016/j.bmcl.2003.10.049
CHEMBL133168 23241 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 315 4 1 3 4.1 COc1ccc(Cn2c(C(=O)O)cc3cc(Cl)ccc32)cc1 10.1016/j.bmcl.2003.10.049
44612708 137434 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753526 137434 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@@H]1CC=C(C(=O)O)[C@@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
57344219 130632 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681880 130632 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 545 8 4 5 4.8 CCOC(=O)c1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
71517574 86385 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313779 86385 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57656921 75211 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036764 75211 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
46842383 8343 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092929 8343 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 530 8 2 4 3.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
72946010 105228 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115104 105228 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71517573 86384 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313778 86384 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 483 4 2 6 2.3 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
57393530 70506 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1946831 70506 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 497 7 3 5 2.5 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44453372 155742 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL405633 155742 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 433 7 2 3 3.4 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
71768798 111099 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 4 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C)(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263257 111099 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 497 4 1 6 3.1 COC1COCCC1N[C@@H]1C[C@H]2OC(C)(C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
9851741 80191 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1021/jm060439n
CHEMBL213601 80191 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1021/jm060439n
67774475 130656 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 488 6 4 4 4.3 Cc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5cccnc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681903 130656 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 488 6 4 4 4.3 Cc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5cccnc45)CC3)C(N)=O)CC2)c1 nan
44444105 94070 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 482 7 0 4 5.5 COc1ccc(/C=C/C(=O)N2CCC(CN3CCC(c4ccc(Cl)cc4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.07.065
CHEMBL249009 94070 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 482 7 0 4 5.5 COc1ccc(/C=C/C(=O)N2CCC(CN3CCC(c4ccc(Cl)cc4)CC3)CC2)cc1OC 10.1016/j.bmcl.2007.07.065
44413158 79969 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 437 8 2 4 3.8 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccco1 10.1016/j.bmcl.2006.04.045
CHEMBL212674 79969 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 437 8 2 4 3.8 CN(C)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccco1 10.1016/j.bmcl.2006.04.045
89823541 126321 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
CHEMBL3650371 126321 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
11699524 95108 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL255499 95108 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 541 7 2 4 5.1 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
11605635 95462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257173 95462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 493 6 2 3 4.9 O=C(/C=C/c1ccc(F)c(F)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11534473 90697 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
CHEMBL239144 90697 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 594 14 1 5 8.0 CCN(CC)CCCC(NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)C(C)C 10.1016/j.bmcl.2006.10.060
54754969 65738 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834632 65738 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 515 6 3 6 4.2 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.08.074
56675205 65793 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834788 65793 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44447783 95074 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 556 6 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255312 95074 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 556 6 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
10325032 95113 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 541 6 1 3 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255513 95113 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 541 6 1 3 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44447782 155311 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 570 7 1 3 7.4 COc1cccc(C2CCN([C@@H]3CC[C@@](C(=O)NCc4cc(C(F)(F)F)cc(C(F)(F)F)c4)(C(C)C)C3)CC2)c1 10.1016/j.bmcl.2007.12.029
CHEMBL403033 155311 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 570 7 1 3 7.4 COc1cccc(C2CCN([C@@H]3CC[C@@](C(=O)NCc4cc(C(F)(F)F)cc(C(F)(F)F)c4)(C(C)C)C3)CC2)c1 10.1016/j.bmcl.2007.12.029
10392978 167457 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL429849 167457 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 558 6 2 5 5.3 CC(C)(O)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cncnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
11421712 74541 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029421 74541 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 568 7 3 7 3.3 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cnccn4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
11365166 74542 None 1 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74542 None 1 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
44593564 187230 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187230 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
22143293 188025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
44453368 97765 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL271725 97765 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
22143309 187939 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496959 187939 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 537 10 4 6 3.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
51039119 176215 None 33 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL2 from CCR2 in human PBMC cellsDisplacement of [125I]-CCL2 from CCR2 in human PBMC cells
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176215 None 33 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-CCL2 from CCR2 in human PBMC cellsDisplacement of [125I]-CCL2 from CCR2 in human PBMC cells
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
53325639 58468 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58468 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
44580591 187857 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL496344 187857 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 9 4 6 3.1 CCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(N)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.07.123
44425649 86127 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL231142 86127 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 554 6 1 2 7.5 C[C@H]1CN(C2CCC(CC3CCC3)(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
22143293 188025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
11700079 149921 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 618 8 3 5 4.5 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
CHEMBL394955 149921 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 618 8 3 5 4.5 CS(=O)(=O)Nc1ccc2[nH]cc(C3CCN(C(C(=O)O)C4CCN(C(=O)/C=C/c5cc(F)c(F)c(F)c5)CC4)CC3)c2c1 10.1021/jm070902b
10129343 173263 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL452509 173263 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 642 11 3 6 5.2 CCN(CC)C(=O)Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@H]1CCCC[C@H]1CS(=O)(=O)c1ccc(SC)cc1 10.1016/j.bmcl.2009.05.041
44425640 96927 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL266017 96927 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 576 5 1 2 7.6 C[C@H]1CN(C2CCC(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44425309 142355 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388867 142355 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc([C@@H](CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
53324942 58676 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684701 58676 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 469 6 1 5 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)c2ccccc2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
60148505 111108 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263268 111108 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 469 4 1 6 2.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
57335017 70336 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70336 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
57391591 70338 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 637 10 4 6 3.8 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944778 70338 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 637 10 4 6 3.8 CC(C)N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
162668957 182758 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4790208 182758 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 495 5 3 7 3.1 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(C)(C)C)nc23)C1=O 10.1021/acsmedchemlett.1c00082
71768900 111112 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 470 4 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2COc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263272 111112 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 470 4 1 6 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2COc3ccc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
10209478 73719 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
CHEMBL2018385 73719 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 551 12 6 5 3.2 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC 10.1016/j.bmcl.2012.03.007
10300284 73730 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018396 73730 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11752457 74537 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
CHEMBL2029417 74537 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
69285563 121226 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
CHEMBL3577936 121226 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 443 8 2 4 3.1 COC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/ml500505q
44442561 93537 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 11 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246399 93537 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 11 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344305 68937 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922797 68937 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
10207591 73415 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2016596 73415 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 507 10 4 4 4.1 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](O)CC(C)(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
44571216 172650 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 757 11 5 8 6.3 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL449674 172650 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 757 11 5 8 6.3 CSc1ccc(C(=O)NC2CCC(NC(=O)OCc3ccccc3)CC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)(C)C)cc1 10.1016/j.bmcl.2008.12.062
67772854 130635 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 7 3 5 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OCCO3)CC1 nan
CHEMBL3681883 130635 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 7 3 5 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)OCCO3)CC1 nan
44415957 81052 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215391 81052 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
22310876 116922 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 396 4 1 4 3.7 CS(=O)(=O)NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL338495 116922 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 396 4 1 4 3.7 CS(=O)(=O)NC(=O)c1cc2ccccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
71519381 86371 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313765 86371 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
49763804 65423 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829616 65423 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 528 7 2 4 4.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(N4CCCC4)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
44571258 183249 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.5 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2008.12.062
CHEMBL479643 183249 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 544 8 3 4 4.5 CN(C)C1CCC(NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(NCc2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2008.12.062
44439163 90292 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238518 90292 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44353447 3773 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
785 3773 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
CHEMBL337246 3773 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2010.02.072
44453234 97469 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270182 97469 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
127025462 137360 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 404 4 1 2 5.9 CC(C)(C)OC[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753005 137360 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 404 4 1 2 5.9 CC(C)(C)OC[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
86767119 129400 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
CHEMBL3671252 129400 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)C12CCOC1CC(NC1CCOCC1)C2 nan
76314242 105251 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115268 105251 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44439163 90292 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238518 90292 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46240482 83575 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204259 83575 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
44447786 95112 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL255511 95112 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 584 7 2 3 7.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3cccc(C(=O)O)c3)CC2)C1 10.1016/j.bmcl.2007.12.029
71768721 111117 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2014.03.036
CHEMBL3263279 111117 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 439 3 1 5 2.7 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCO[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2014.03.036
122178127 121218 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 541 12 4 4 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CCc2ccccc2)c(C)c1 10.1021/ml500505q
CHEMBL3577928 121218 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 541 12 4 4 4.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)CCc2ccccc2)c(C)c1 10.1021/ml500505q
72946202 105238 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 496 5 1 6 2.5 CCN1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115114 105238 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 496 5 1 6 2.5 CCN1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
54755083 65742 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834636 65742 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
44425636 85946 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230078 85946 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 590 6 1 2 8.0 C[C@H]1CN(C2CCC(CC3CC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573412 187425 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1007/s00044-010-9501-4
CHEMBL493780 187425 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1007/s00044-010-9501-4
44453565 169005 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439252 169005 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2Cl)C1 10.1016/j.bmcl.2008.02.015
10138789 166507 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL427875 166507 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
44573535 187436 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1007/s00044-010-9501-4
CHEMBL493843 187436 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1007/s00044-010-9501-4
44573535 187436 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493843 187436 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 528 6 2 4 4.7 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCS(=O)(=O)CC2)C1 10.1016/j.bmcl.2008.12.050
11563597 91951 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL241462 91951 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
11563597 91951 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241462 91951 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 632 13 1 4 8.7 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57344315 68939 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 nan
CHEMBL1922799 68939 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 530 8 2 5 3.9 COc1ccc(C2CCC(NC(C(N)=O)C3CCN(C(=O)/C=C/c4cc(F)c(F)c(F)c4)CC3)CC2)cn1 nan
72947595 105219 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115096 105219 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 511 4 2 6 1.5 COC1COCCC1N[C@@H]1C[C@H]2CN(C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656713 75203 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036756 75203 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 488 7 1 3 5.5 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CCCc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
11711078 75218 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036773 75218 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 400 4 1 4 2.9 CCN1CCO[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10183362 73703 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018369 73703 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 465 10 4 4 3.1 CC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
10392559 155037 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccnnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
CHEMBL401609 155037 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor in human monocytesDisplacement of [125I]MCP1 from CCR2 receptor in human monocytes
ChEMBL 542 6 1 4 6.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CCC(c3ccnnc3)CC2)C1 10.1016/j.bmcl.2007.12.029
44425637 85985 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230405 85985 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 604 6 1 2 8.4 C[C@H]1CN([C@@H]2CC[C@](CC3CCC3)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
44573412 187425 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL493780 187425 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 478 6 2 2 6.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCCCC2)C1 10.1016/j.bmcl.2008.12.050
24801523 97853 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97853 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22310972 116776 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2c(-c3ccccc3)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337720 116776 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2c(-c3ccccc3)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44395092 127285 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 522 8 4 7 2.9 Cc1csc(C(=O)NNC(=O)CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL365853 127285 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 522 8 4 7 2.9 Cc1csc(C(=O)NNC(=O)CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)c1 10.1016/j.bmcl.2004.08.008
10208555 73710 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018376 73710 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1016/j.bmcl.2012.03.007
10208555 73710 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1021/ml500505q
CHEMBL2018376 73710 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperatureInhibition of [125I]hMCP1 binding to CCR2 in human PBMC incubated for 30 mins at room temperature
ChEMBL 527 11 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)Cc2ccccc2)c(C)c1 10.1021/ml500505q
44395201 66419 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 8 2 3 3.5 O=C(CCNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL185190 66419 None 0 Human Binding pIC50 = 4.2 4.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 413 8 2 3 3.5 O=C(CCNC(=O)c1ccccc1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
57344313 130655 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
CHEMBL3681902 130655 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 503 7 3 4 4.1 NC(=O)C(NC1CCC(c2c[nH]c3ccncc23)CC1)C1CCN(C(=O)/C=C/c2ccc(F)cc2)CC1 nan
44415927 80853 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215271 80853 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 512 9 1 2 6.8 C=CC[C@H](CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44453473 155537 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 464 6 3 4 2.8 Nc1ccc(Br)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL404260 155537 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 464 6 3 4 2.8 Nc1ccc(Br)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
25008678 94150 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249414 94150 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 486 7 1 3 6.2 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(Cl)cc(Cl)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11570431 91980 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL241502 91980 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 564 13 1 4 7.9 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44439173 90705 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 650 13 1 4 8.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.10.060
CHEMBL239145 90705 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 650 13 1 4 8.8 CCN(CC)CCCC(C)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.10.060
52947417 19306 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN(C2CCN(c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290522 19306 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 490 6 3 5 2.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN(C2CCN(c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
72946199 105231 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115107 105231 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 610 6 1 8 3.0 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10206007 73706 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018372 73706 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 479 10 4 4 3.3 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@@H](O)C(C)C)c(C)c1 10.1016/j.bmcl.2012.03.007
11237168 74529 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 489 6 3 4 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029409 74529 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 489 6 3 4 3.5 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10302973 93550 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246415 93550 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 4 3.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44442589 93769 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 607 11 5 6 4.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247439 93769 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 607 11 5 6 4.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)OC(C)C)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44423281 142113 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C1CCC(N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
CHEMBL388308 142113 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 498 5 1 2 6.4 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C1CCC(N2CCC(c3ccccc3)CC2)C1 10.1021/jm070166b
44425641 86064 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230832 86064 None 0 Mouse Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
86698129 126302 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650352 126302 None 0 Human Binding pIC50 = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
46240481 83584 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 477 6 3 6 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml300260s
CHEMBL2204269 83584 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 477 6 3 6 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncnc3)CC2)C1 10.1021/ml300260s
56668313 65789 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 535 8 2 7 4.5 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C4CCCC4)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834784 65789 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 535 8 2 7 4.5 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C4CCCC4)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
44353370 23764 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 330 4 1 4 3.9 O=C(O)c1cc2cc(Cl)ccc2n1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2003.10.049
CHEMBL133569 23764 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 330 4 1 4 3.9 O=C(O)c1cc2cc(Cl)ccc2n1Cc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2003.10.049
11678573 90637 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238936 90637 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
53324141 58465 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683070 58465 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 511 7 1 5 4.3 CCO[C@H]1COCC[C@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
11340816 74533 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 491 6 3 6 2.2 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ncccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029413 74533 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 491 6 3 6 2.2 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ncccn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
10182382 93960 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL248418 93960 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 450 9 4 4 1.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(N)=O)c(C)c1 10.1016/j.bmcl.2007.07.028
11678573 90637 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL238936 90637 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 566 13 1 5 7.4 CCN(CC)CCCC(C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44395055 64502 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL181432 64502 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
44415995 80050 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL212972 80050 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
23656260 89070 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 501 7 2 4 4.8 COc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
CHEMBL236509 89070 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 501 7 2 4 4.8 COc1ccc(/C=C/C(=O)N2CCC(C(C(=O)O)N3CCC(c4c[nH]c5ccccc45)CC3)CC2)cc1 10.1021/jm070902b
46842382 8341 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092920 8341 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
508744 66213 None 1 Human Binding pIC50 = 4.2 4.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL184474 66213 None 1 Human Binding pIC50 = 4.2 4.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 7 2 3 2.9 O=C(CNC(=O)c1ccccc1)NCC1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
127025160 137423 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 429 3 1 3 4.6 C[C@H]1CC=C(C(=O)NS(=O)(=O)C(F)(F)F)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753428 137423 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 429 3 1 3 4.6 C[C@H]1CC=C(C(=O)NS(=O)(=O)C(F)(F)F)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
57344316 68932 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922792 68932 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 554 7 4 4 5.0 O=C(NO)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344230 130640 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)cc2)CC1 nan
CHEMBL3681888 130640 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 491 6 4 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)cc2)CC1 nan
11080 29083 None 79 Human Binding pIC50 = 5.2 5.2 -1 6
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29083 None 79 Human Binding pIC50 = 5.2 5.2 -1 6
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
9851741 80191 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213601 80191 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 604 7 1 2 8.0 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425654 86228 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231247 86228 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 532 5 1 3 6.4 CS[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53321484 58475 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683080 58475 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 510 7 1 6 3.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](CC2CC2)(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)C1 10.1016/j.bmcl.2011.01.015
44442580 93545 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 4 6 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.07.028
CHEMBL246409 93545 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 537 10 4 6 2.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1[N+](=O)[O-] 10.1016/j.bmcl.2007.07.028
44413310 138957 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 10 2 3 5.0 CCN(CC)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL378517 138957 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 10 2 3 5.0 CCN(CC)CCNC(C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
72948004 105256 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115273 105256 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57656719 75214 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036767 75214 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1ccc(C(F)(F)F)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
54580189 62567 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 505 6 1 8 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)ns3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782575 62567 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 505 6 1 8 2.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)ns3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
23656433 88761 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cccc(Cl)c2Cl)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236269 88761 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cccc(Cl)c2Cl)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
72945830 105225 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115101 105225 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 526 4 1 7 2.2 COC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67220645 75228 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036783 75228 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 2 2 4 1.6 CN1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
127027955 137251 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 278 2 1 1 4.3 Cc1cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)ccc1Cl 10.1016/j.bmcl.2015.11.051
CHEMBL3751958 137251 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 278 2 1 1 4.3 Cc1cc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)ccc1Cl 10.1016/j.bmcl.2015.11.051
44415898 81119 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL215654 81119 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
11478362 73805 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 547 11 4 4 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018532 73805 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 547 11 4 4 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
44453592 160053 None 24 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL410829 160053 None 24 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 405 6 2 3 2.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2)C1 10.1016/j.bmcl.2008.02.015
44442582 93547 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1C 10.1016/j.bmcl.2007.07.028
CHEMBL246411 93547 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 536 10 4 5 3.3 COc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1C 10.1016/j.bmcl.2007.07.028
9952114 124382 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)NC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL363908 124382 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 385 6 2 3 2.8 Cc1cccc(C(=O)NCC(=O)NC2CCN(Cc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
71518408 86401 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 449 3 1 3 5.2 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314058 86401 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 449 3 1 3 5.2 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCCCCC1)C2 10.1016/j.bmcl.2012.10.069
54772206 86588 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 514 7 2 7 4.0 COc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
CHEMBL2315930 86588 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 514 7 2 7 4.0 COc1cnccc1[C@H]1CC[C@@H](N2CC(NC(=O)CNc3ncnc4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2012.12.017
54772204 86590 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 500 6 3 7 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315932 86590 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 500 6 3 7 3.7 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2012.12.017
54772205 86593 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 4.3 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3O)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315935 86593 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 499 6 3 6 4.3 O=C(CNc1ncnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3ccccc3O)CC2)C1 10.1016/j.bmcl.2012.12.017
72663455 129399 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129399 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
11599317 95558 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
CHEMBL257628 95558 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 555 7 2 4 6.0 COc1ccc2[nH]cc(C3CCN(C(CO)C4CCN(C(=O)/C=C/c5ccc(Cl)c(Cl)c5)CC4)CC3)c2c1 10.1016/j.bmcl.2008.05.010
53324304 58462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683067 58462 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 497 6 1 5 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
10228435 73715 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
CHEMBL2018381 73715 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 494 11 5 5 3.1 CCC[C@@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2012.03.007
46927117 65426 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829619 65426 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
56661451 65796 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834791 65796 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 500 6 2 6 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44573699 187672 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL495151 187672 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 508 6 2 3 5.8 CC1COCC(C)C1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
11306757 73735 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018401 73735 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 508 12 5 5 4.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
57391765 71013 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
CHEMBL1951774 71013 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cccnn3)CC2)C1 10.1021/ml200030q
44425244 151802 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 594 7 2 5 6.6 Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL396517 151802 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 594 7 2 5 6.6 Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
23630215 62542 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782376 62542 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 508 5 1 5 4.3 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2C3CCCC2COC3)C1 10.1016/j.bmcl.2011.01.034
10120067 73727 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018393 73727 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 550 12 5 5 4.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(C)(C)C 10.1016/j.bmcl.2012.03.007
52943756 19288 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19288 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counter
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44425274 150856 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 640 10 2 5 7.4 CC(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL395721 150856 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 640 10 2 5 7.4 CC(C)C(=O)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
24801690 98039 None 25 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98039 None 25 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to wild type CCR2Binding affinity to wild type CCR2
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44425647 86099 None 0 Mouse Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86099 None 0 Mouse Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44423282 85272 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 522 4 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
CHEMBL226017 85272 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytesDisplacement of [125]hMCP1 from human CCR2 receptor expressed in human monocytes
ChEMBL 522 4 1 2 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H]1CC[C@@H](N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm070166b
162648673 179948 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 522 6 3 7 3.4 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(OC(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
CHEMBL4746510 179948 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human PBMC measured after 30 mins by Microscintillation counting analysis
ChEMBL 522 6 3 7 3.4 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(OC(F)(F)F)cc23)C1=O 10.1021/acsmedchemlett.1c00082
44425633 86039 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230721 86039 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 578 5 1 2 7.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44570718 183831 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480621 183831 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
11621035 154666 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 559 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(Cl)ccc23)CC1 10.1021/jm070902b
CHEMBL399616 154666 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 559 6 2 3 5.8 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3cc(Cl)ccc23)CC1 10.1021/jm070902b
10052388 187550 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1007/s00044-010-9501-4
CHEMBL494541 187550 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 520 7 2 3 5.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C2CC2)C1 10.1007/s00044-010-9501-4
57391768 71011 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
CHEMBL1951772 71011 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counterDisplacement of [125I]MCP1 from CCR2 in human PBMC after 30 mins by gamma counter
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3ccncn3)CC2)C1 10.1021/ml200030q
44573608 187549 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494540 187549 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 522 8 2 3 6.3 CCCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
11180383 77621 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088211 77621 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity to CCR2Binding affinity to CCR2
ChEMBL 550 8 2 5 4.6 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)Cc2nc3cccc(C(F)(F)F)c3[nH]2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
22143294 193424 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 193424 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
49763686 65422 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829615 65422 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
508750 168533 None 1 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL435499 168533 None 1 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
127028586 137505 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 264 2 1 1 4.0 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3754119 137505 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 264 2 1 1 4.0 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)cc2)C1 10.1016/j.bmcl.2015.11.051
11844468 139594 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
CHEMBL379742 139594 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 9 1 2 8.3 C[C@@H]1CN(CC[C@H](CNCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC[C@@H]1c1ccccc1 10.1021/jm060439n
44395088 67169 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL187701 67169 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 514 8 1 5 4.2 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2004.08.008
10209102 93536 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 540 11 4 4 3.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL246398 93536 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 540 11 4 4 3.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NCc2ccccc2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344320 130641 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 527 6 4 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681889 130641 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 527 6 4 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2cc(F)c(F)c(F)c2)CC1 nan
72948001 105220 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115097 105220 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
46241611 83563 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
CHEMBL2204247 83563 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 506 7 3 6 2.5 COc1cccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)n1 10.1021/ml300260s
57344232 130642 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 519 7 4 4 5.3 CSc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
CHEMBL3681890 130642 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 519 7 4 4 5.3 CSc1cccc(NC(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)c1 nan
44395126 65411 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL182958 65411 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44395126 65411 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL182958 65411 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 494 8 2 6 3.6 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3ccccc3)c3cccc(O)c3)CC2)cc1 10.1016/j.bmcl.2004.08.009
57656915 75217 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 342 4 1 3 2.7 O=C(Nc1ccccc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036772 75217 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 342 4 1 3 2.7 O=C(Nc1ccccc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
11341950 73804 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 557 11 4 4 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(Br)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018531 73804 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 557 11 4 4 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(Br)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
42632836 93384 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2cc(Cl)cc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245696 93384 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2cc(Cl)cc(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
68004094 86599 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1ccnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
CHEMBL2315941 86599 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 505 6 3 7 3.8 O=C(CNc1ccnc2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1016/j.bmcl.2012.12.017
57396900 70520 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 399 6 2 3 3.2 CC(C)N(C)[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
CHEMBL1947040 70520 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 399 6 2 3 3.2 CC(C)N(C)[C@H]1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2011.12.057
44416041 80430 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL214647 80430 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 530 8 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC(c2ccc(F)cc2)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
44416015 81131 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215689 81131 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 538 7 1 2 7.1 CC(C)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
44413144 139217 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL378784 139217 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44413144 139217 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL378784 139217 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1021/jm060439n
23656434 89616 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cc(Cl)cc(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL237538 89616 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 528 5 3 3 6.1 O=C(O)C(C1CCN(C(=O)Nc2cc(Cl)cc(Cl)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
44442569 93733 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 6 2.0 CC(C)(C)NC(=O)[C@H](CNCc1ccc(S(C)(=O)=O)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247213 93733 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 556 10 4 6 2.0 CC(C)(C)NC(=O)[C@H](CNCc1ccc(S(C)(=O)=O)cc1)NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2007.07.028
44415958 80497 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
CHEMBL214747 80497 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 578 7 1 2 8.0 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(C=Cc3ccccc32)CC1)C1CCCCC1 10.1016/j.bmcl.2006.07.011
11563451 151916 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL396621 151916 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44453533 97878 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 420 6 3 4 2.7 Nc1ccc(Cl)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272330 97878 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 420 6 3 4 2.7 Nc1ccc(Cl)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10008367 2020 None 50 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2020 None 50 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2020 None 50 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2020 None 50 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of rat CCR2Inhibition of rat CCR2
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
11563451 151916 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL396621 151916 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44425321 86134 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
CHEMBL231150 86134 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 740 10 2 5 9.0 CC(C(=O)Nc1nc(C(CCN2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1)c1ccccc1 10.1016/j.bmcl.2006.10.059
44425651 143175 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL389610 143175 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
56643545 130622 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
CHEMBL3681871 130622 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 520 7 3 3 4.9 NC(=O)C(N[C@H]1CC[C@@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 nan
10025168 66984 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL186855 66984 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.008
10025168 66984 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL186855 66984 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 420 5 2 5 2.7 Cc1csc(C(=O)NNC(=O)CN2CCCN(Cc3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2004.08.009
44395036 125050 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL364405 125050 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 399 7 2 3 3.2 O=C(CCNC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
127027625 137252 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 366 2 1 1 5.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3751959 137252 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 366 2 1 1 5.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
22143293 188025 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497577 188025 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 495 8 5 6 2.4 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
57343816 130625 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3681874 130625 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cccc(C(F)(F)F)c2)CC1 nan
53320974 58690 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 464 4 1 4 2.8 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)N2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684715 58690 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 30 mins by human whole cell binding assay
ChEMBL 464 4 1 4 2.8 CC(C)[C@]1(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)N2CCCCC2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2011.01.052
57344314 68928 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922788 68928 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 553 7 2 4 5.7 COC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44442564 93538 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
CHEMBL246400 93538 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 492 9 4 4 2.9 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1 10.1016/j.bmcl.2007.07.028
46842236 7865 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089849 7865 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 598 8 2 4 4.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
44413411 77736 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2006.04.045
CHEMBL209002 77736 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.4 CC1CCN(CCN[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2)CC1 10.1016/j.bmcl.2006.04.045
44453507 168976 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL439062 168976 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 531 7 2 3 5.6 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccccc2-c2ccc3ccccc3c2)C1 10.1016/j.bmcl.2008.02.015
69286108 121231 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
CHEMBL3577941 121231 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 505 9 2 4 4.5 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](COc2ccccc2)C1 10.1021/ml500505q
71518574 86389 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313784 86389 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 467 4 1 5 3.3 COC1COCCC1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
89823496 126313 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
CHEMBL3650363 126313 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
89823439 126297 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650347 126297 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
44573568 187468 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1007/s00044-010-9501-4
CHEMBL494019 187468 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1007/s00044-010-9501-4
44439164 90771 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239169 90771 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
44439164 90771 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL239169 90771 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 610 13 4 7 5.1 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44573650 193208 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL523503 193208 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 564 6 3 4 5.2 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2(O)C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
10323468 187670 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1007/s00044-010-9501-4
CHEMBL495149 187670 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 494 6 2 3 5.7 CC1CC(N[C@@H]2CC[C@@](C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)(C(C)C)C2)CCO1 10.1007/s00044-010-9501-4
72948001 105220 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115097 105220 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 525 4 2 6 1.8 CNC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44573568 187468 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494019 187468 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.bmcl.2008.12.050
72947593 105236 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115112 105236 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44413144 139217 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
CHEMBL378784 139217 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 465 8 2 3 4.4 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccc(F)cc1 10.1016/j.bmcl.2006.04.045
44442544 93764 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.6 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247407 93764 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 520 10 4 4 3.6 Cc1ccc(CNCC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
44353190 116564 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL336421 116564 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 349 4 1 3 4.7 COc1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
46240785 83580 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
CHEMBL2204264 83580 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 510 7 3 6 3.1 CCc1ncc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)s1 10.1021/ml300260s
72947593 105236 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115112 105236 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 468 4 2 6 1.7 COC1COCCC1N[C@@H]1C[C@H]2CNC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
70692344 75196 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036749 75196 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 370 3 2 3 3.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(CC2CCCNC2)CC1 10.1016/j.bmcl.2012.04.118
11844083 77991 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 581 8 1 3 6.9 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCN1c1ccccc1 10.1021/jm060439n
CHEMBL209696 77991 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 581 8 1 3 6.9 CC1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CCN1c1ccccc1 10.1021/jm060439n
44395238 123843 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CN2CCC(NCc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
CHEMBL362536 123843 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 406 6 3 5 2.3 Cc1csc(C(=O)NNC(=O)CN2CCC(NCc3ccc(Cl)cc3)C2)c1 10.1016/j.bmcl.2004.08.009
42632830 93383 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL245694 93383 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)cc2Cl)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
44416156 81150 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 657 8 1 4 6.1 CS(=O)(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL215768 81150 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 657 8 1 4 6.1 CS(=O)(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
24801345 97852 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
CHEMBL272167 97852 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to CCR2 E291A mutantBinding affinity to CCR2 E291A mutant
ChEMBL 475 6 3 3 3.9 Cc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)c(C)c1 10.1021/jm701488f
44453171 95735 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL258364 95735 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 449 6 2 3 3.2 O=C(CNC(=O)c1cccc(Br)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10300705 97896 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 5.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1Cl 10.1021/jm701488f
CHEMBL272407 97896 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 501 7 3 3 5.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1Cl 10.1021/jm701488f
53325639 58468 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683073 58468 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometryDisplacement of MCP-Alexa 488 from CCR2 in human whole blood after 5 mins by flow cytometry
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.015
57402059 70340 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944780 70340 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PMBCDisplacement of [125I]MCP-1 from CCR2 in human PMBC
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
44425319 86333 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL231340 86333 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 727 10 2 6 7.9 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3ccccn3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
46241011 83573 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 483 6 3 7 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204257 83573 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysisDisplacement of [125I]-MCP-1 from CCR2 in human THP-1 cells after 2 hrs by microplate scintillation and luminescence counter analysis
ChEMBL 483 6 3 7 1.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nncs3)CC2)C1 10.1021/ml300260s
44444114 94207 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 6 1 2 5.4 O=C(/C=C/c1cc(F)cc(F)c1)NC1CCC(CN2CCC(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2007.07.065
CHEMBL249811 94207 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 460 6 1 2 5.4 O=C(/C=C/c1cc(F)cc(F)c1)NC1CCC(CN2CCC(c3ccc(F)c(F)c3)CC2)C1 10.1016/j.bmcl.2007.07.065
24801180 98038 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL273079 98038 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
122181145 121831 None 0 Mouse Binding pIC50 = 5.1 5.1 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589840 121831 None 0 Mouse Binding pIC50 = 5.1 5.1 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 528 6 1 3 6.1 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
44395232 66996 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 1 6 3.9 COc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
CHEMBL186913 66996 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 508 9 1 6 3.9 COc1cccc(C(O)(CCN2CCCN(Cc3ccc(S(C)(=O)=O)cc3)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.08.008
71518727 86405 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 451 3 1 4 4.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314064 86405 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 451 3 1 4 4.1 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCCC[C@@H]1C[C@@H](NC1CCOCC1)C2 10.1016/j.bmcl.2012.10.069
57656808 75221 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 4 2 4 2.4 CCN1CCNC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036776 75221 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 399 4 2 4 2.4 CCN1CCNC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
54768838 86595 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1nc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
CHEMBL2315937 86595 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation countingAntagonist activity against human CCR2 in human THP1 cells using [I125]MCP-1 by scintillation counting
ChEMBL 520 6 3 8 3.5 Cc1nc(NCC(=O)NC2CN([C@H]3CC[C@@](O)(c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc2n1 10.1016/j.bmcl.2012.12.017
57344295 130623 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681872 130623 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 541 6 4 3 5.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
57344303 130646 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130646 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44425635 153530 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL398000 153530 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 592 6 1 2 8.2 CC(C)C[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44413076 140146 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 9 1 3 5.0 CN(C)CCCN(C)[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL380258 140146 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 475 9 1 3 5.0 CN(C)CCCN(C)[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
44425652 168766 None 0 Mouse Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168766 None 0 Mouse Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
10312346 188460 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502795 188460 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 614 9 3 6 4.4 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N(C)C)cc1 10.1016/j.bmcl.2009.05.041
50991056 62564 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782572 62564 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)cnn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10218843 172784 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451340 172784 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of [125I]MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425651 143175 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL389610 143175 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 530 6 1 3 6.0 COCC1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
53319664 58675 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
CHEMBL1684700 58675 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated 1 hrs by human whole cell binding assay
ChEMBL 461 6 1 5 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C2CCCC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.052
53322810 58470 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683075 58470 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44593561 12661 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL1187238 12661 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494580 12661 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 452 6 2 3 4.5 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2COC2)C1 10.1016/j.bmcl.2008.12.050
71768689 111109 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263269 111109 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Antagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxisAntagonist activity at human CCR2 expressed in THP1 cells assessed as inhibition of MCP-1 induced chemotaxis
ChEMBL 469 4 1 6 2.3 CO[C@H]1COCC[C@H]1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2014.03.036
22143346 172649 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
CHEMBL449672 172649 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 634 11 4 6 4.5 CCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)C1 10.1016/j.bmcl.2008.07.123
54580188 62565 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782573 62565 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
11606702 145752 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
CHEMBL391662 145752 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.ejmech.2010.04.024
44449175 95504 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 552 7 2 3 5.2 CC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257351 95504 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 552 7 2 3 5.2 CC(=O)NCC(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2008.05.010
49763685 65421 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 7 2 5 3.7 COC(=O)c1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829614 65421 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 517 7 2 5 3.7 COC(=O)c1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2011.06.080
44612590 137468 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3753813 137468 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 298 2 1 1 4.7 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(Cl)c2)C1 10.1016/j.bmcl.2015.11.051
44415899 80072 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL213058 80072 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CC[C@@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
11844212 98647 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
CHEMBL277279 98647 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2006.07.011
44415995 80050 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
CHEMBL212972 80050 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 621 7 1 3 6.7 CC(=O)N1CCCC(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2006.07.011
25007995 154869 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL400680 154869 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@@H]3CC[C@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
11844212 98647 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL277279 98647 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 590 7 1 2 7.7 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm060439n
11662833 89186 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 471 6 2 3 4.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
CHEMBL236721 89186 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of human CCR2Inhibition of human CCR2
ChEMBL 471 6 2 3 4.8 O=C(O)C(C1CCN(C(=O)/C=C/c2ccccc2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1021/jm070902b
122181235 121848 None 0 Mouse Binding pIC50 = 5.1 5.1 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589949 121848 None 0 Mouse Binding pIC50 = 5.1 5.1 - 0
Antagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assayAntagonist activity against mouse CCR2B expressed in human U2OS cells co-expressing beta-arrestin assessed as inhibition of mouse CCL2-induced beta-arrestin recruitment pre-incubated for 10 mins before mouse CCL2 stimulation for 90 mins by luminescence based assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
44416125 80919 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 569 7 2 4 5.5 COC(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215333 80919 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 569 7 2 4 5.5 COC(=O)NC(CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
57344300 130643 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 509 6 4 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)c(F)c2)CC1 nan
CHEMBL3681891 130643 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 509 6 4 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)Nc2ccc(F)c(F)c2)CC1 nan
71517577 86368 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313762 86368 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 1 6 2.9 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](N(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
76314234 105221 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115098 105221 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 553 5 2 6 2.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)NC(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
44425318 150309 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL395289 150309 None 0 Mouse Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 732 10 2 6 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)Cc3cccs3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
90656021 111114 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2nccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
CHEMBL3263274 111114 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of labeled MCP-1 from human CCR2 expressed in THP1 cellsDisplacement of labeled MCP-1 from human CCR2 expressed in THP1 cells
ChEMBL 511 5 1 8 1.6 COC1COCCC1N[C@@H]1C[C@H]2OCC[C@@]2(C(=O)N2CC3CC2CN3c2nccc(C(F)(F)F)n2)C1 10.1016/j.bmcl.2014.03.036
89823460 126337 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650387 126337 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)cc(C(F)(F)F)c2)C1 nan
72946200 105230 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115106 105230 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 570 7 1 8 2.2 COCCOC(=O)N1C[C@@H]2C[C@@H](NC3CCOCC3OC)C[C@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
56668309 65774 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834718 65774 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 558 6 3 8 3.6 NC(=O)n1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4ccc5c(c4)OCO5)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
127028591 137452 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.8 Cc1ccc([C@]2(C)CCCC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
CHEMBL3753683 137452 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.8 Cc1ccc([C@]2(C)CCCC=C2C(=O)O)cc1C 10.1016/j.bmcl.2015.11.051
89823691 126316 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 526 5 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2F)C1 nan
CHEMBL3650366 126316 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 526 5 1 6 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)c2F)C1 nan
11843812 79902 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL212423 79902 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1016/j.bmcl.2006.04.045
57344307 130649 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccncc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681897 130649 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 539 7 3 4 4.4 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccncc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
89823344 126348 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650397 126348 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
11843812 79902 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1021/jm060439n
CHEMBL212423 79902 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 563 9 2 3 6.6 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCC(c2ccccc2)CC1)c1ccccc1 10.1021/jm060439n
89823453 126355 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 464 3 0 5 3.2 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCOCC1)C2 nan
CHEMBL3650403 126355 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 464 3 0 5 3.2 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCOCC1)C2 nan
508729 95533 None 1 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257510 95533 None 1 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 416 7 2 5 2.4 O=C(CNC(=O)c1cccc([N+](=O)[O-])c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
46884855 8301 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092656 8301 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
44413399 79527 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
CHEMBL211404 79527 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 501 8 2 3 5.5 CC1CCCCN1CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2006.04.045
70687886 74528 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 487 6 1 3 4.7 CN([C@H]1CC[C@@H](c2ccccc2)CC1)[C@H]1CCN(C(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1021/ml200199c
CHEMBL2029408 74528 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 487 6 1 3 4.7 CN([C@H]1CC[C@@H](c2ccccc2)CC1)[C@H]1CCN(C(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1021/ml200199c
44573451 187565 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1007/s00044-010-9501-4
CHEMBL494591 187565 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 (unknown origin)Antagonist activity at CCR2 (unknown origin)
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1007/s00044-010-9501-4
25008849 94178 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL249609 94178 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 472 7 1 3 5.3 COc1ccc(C2CCN(C[C@H]3CC[C@@H](NC(=O)/C=C/c4cc(F)c(F)c(F)c4)C3)CC2)cc1 10.1016/j.bmcl.2007.07.065
46945255 65434 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1016/j.bmcl.2011.06.080
CHEMBL1829627 65434 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence countingDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 2 hrs by microplate scintillation and luminescence counting
ChEMBL 475 6 3 5 2.9 Nc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1016/j.bmcl.2011.06.080
44573451 187565 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494591 187565 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cellsDisplacement of [125I]hMCP1 from human CCR2 receptor expressed in CHO cells
ChEMBL 466 6 2 3 4.9 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOC2)C1 10.1016/j.bmcl.2008.12.050
11690139 75223 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036778 75223 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 412 3 1 3 3.4 CCN1CCC[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
44415957 81052 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
CHEMBL215391 81052 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2006.07.011
70683619 74526 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029406 74526 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 473 6 2 3 4.4 O=C(NCC(=O)N1CC[C@@H](N[C@H]2CC[C@@H](c3ccccc3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
22310850 116805 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2cc(-c3ccccc3)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL337857 116805 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 395 4 1 2 6.4 O=C(O)c1cc2cc(-c3ccccc3)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
44413137 78890 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2006.04.045
CHEMBL211292 78890 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 453 8 2 4 4.3 CN(C)CCN[C@@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1cccs1 10.1016/j.bmcl.2006.04.045
72947191 105258 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115275 105258 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 600 7 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)CCc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
67774197 130650 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
CHEMBL3681898 130650 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 542 6 4 4 5.3 NC(=O)C(NC1CCC(c2c[nH]c3cccnc23)CC1)C1CCN(C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 nan
72946013 105257 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115274 105257 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to CCR2 receptor (unknown origin)Binding affinity to CCR2 receptor (unknown origin)
ChEMBL 560 4 1 6 2.4 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)C#CC3CC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10207542 73717 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 506 9 5 5 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C2(O)CCCC2)c(C)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018383 73717 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 506 9 5 5 3.2 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C2(O)CCCC2)c(C)c1 10.1016/j.bmcl.2012.03.007
24801524 167326 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 525 7 3 5 2.7 CS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL429425 167326 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 525 7 3 5 2.7 CS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
22268768 154919 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 10 5 5 2.4 CCNC(=O)C(C)(CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2007.07.028
CHEMBL400968 154919 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 507 10 5 5 2.4 CCNC(=O)C(C)(CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1N 10.1016/j.bmcl.2007.07.028
44395066 124461 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 8 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL363994 124461 None 0 Human Binding pIC50 = 4.1 4.1 - 0
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2BConcentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
ChEMBL 398 8 1 3 4.5 O=C(CCCC(=O)c1ccccc1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
71518570 86402 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 453 3 1 4 4.4 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCSCC1)C2 10.1016/j.bmcl.2012.10.069
CHEMBL2314059 86402 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 453 3 1 4 4.4 O=C(N1CCc2ncc(C(F)(F)F)cc2C1)[C@@]12CCC[C@@H]1C[C@@H](NC1CCSCC1)C2 10.1016/j.bmcl.2012.10.069
72948004 105256 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115273 105256 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 578 5 1 6 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)/C=C/C(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
71716742 86382 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313776 86382 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 510 5 2 6 2.0 COC1COCCC1N[C@@H]1C[C@H]2C[C@H](C(N)=O)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
44453471 97868 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272283 97868 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 470 7 3 5 2.9 Nc1ccc(OC(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
10228205 93726 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 10 4 4 2.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247205 93726 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 490 10 4 4 2.6 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CC2)c(C)c1 10.1016/j.bmcl.2007.07.028
57344303 130646 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681894 130646 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 538 7 3 3 5.0 NC(=O)C(N[C@H]1CC[C@H](c2c[nH]c3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57402059 70340 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944780 70340 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human THP1 cellsDisplacement of [125I]MCP-1 from CCR2 in human THP1 cells
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
25268795 148505 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 4.7 C[N+](C)(Cc1ccc(CNC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL393835 148505 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 421 6 1 2 4.7 C[N+](C)(Cc1ccc(CNC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
86767120 129401 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671253 129401 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 468 4 1 5 2.9 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)C1 nan
44449081 95511 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 535 6 2 3 5.4 O=C(/C=C/c1cccc(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL257385 95511 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 535 6 2 3 5.4 O=C(/C=C/c1cccc(Br)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11634928 168889 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 514 5 3 3 6.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
CHEMBL438353 168889 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Binding affinity at human CCR2 receptorBinding affinity at human CCR2 receptor
ChEMBL 514 5 3 3 6.0 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/j.bmcl.2008.05.010
11606702 145752 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL391662 145752 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 580 14 1 5 7.8 CCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
56671794 65795 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834790 65795 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44595711 137319 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137319 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
44416157 80593 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL215020 80593 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 564 8 1 2 7.5 C[C@H]1CN(CC[C@H](CC2CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425630 86025 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL230617 86025 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 I40L mutant expressed in CHO cells
ChEMBL 550 4 1 2 7.2 C[C@H]1CN([C@@H]2CC[C@](C)(C(=O)NCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
11330529 74538 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029418 74538 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 567 7 3 6 3.9 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4cccnc4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
24801689 97792 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97792 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
44425242 86041 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 588 8 2 5 6.6 Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230727 86041 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 expressed in monocytesDisplacement of [125I]MCP1 from human CCR2 expressed in monocytes
ChEMBL 588 8 2 5 6.6 Nc1nc(C(CCN2CCC(c3ccc(F)cc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
54583186 62570 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782578 62570 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 496 6 1 5 4.3 CCC1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
10232019 73728 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
CHEMBL2018394 73728 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 584 14 5 5 5.1 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NCc1ccccc1 10.1016/j.bmcl.2012.03.007
53322811 58472 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683077 58472 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 484 6 1 6 3.1 CC[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N[C@H]2CCOC[C@H]2OC)C1 10.1016/j.bmcl.2011.01.015
54586021 62541 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782375 62541 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assayDisplacement of [125I]MCP1 from human CCR2 preincubated for 30 mins by human whole cell binding assay
ChEMBL 494 4 0 5 4.1 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](N2CCC3COCCC32)C1 10.1016/j.bmcl.2011.01.034
10008367 2020 None 50 Mouse Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
777 2020 None 50 Mouse Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL1289316 2020 None 50 Mouse Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
CHEMBL2426341 2020 None 50 Mouse Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counterDisplacement of [125I]MCP1 from mouse CCR2 after 30 mins by gamma counter
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2 10.1016/j.bmcl.2010.10.020
10281715 73721 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
CHEMBL2018387 73721 None 0 Human Binding pIC50 = 8 8.0 - 0
Antagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degCAntagonist activity against CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis at 37 degC
ChEMBL 579 13 6 5 4.0 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)NC(C)C 10.1021/ml500505q
22143146 183904 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183904 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]MCP1 from CCR2 in human PBMCsDisplacement of [125I]MCP1 from CCR2 in human PBMCs
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
76314242 105251 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115268 105251 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 544 5 1 6 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(c3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11633080 93630 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 1 6.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CC2CCC1C2 10.1016/j.bmcl.2007.01.115
CHEMBL246728 93630 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 417 5 1 1 6.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CC2CCC1C2 10.1016/j.bmcl.2007.01.115
44442591 93811 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 631 11 5 5 4.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247635 93811 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 631 11 5 5 4.8 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)C(=O)NC(C)(C)C)c(C)c1 10.1016/j.bmcl.2007.07.028
22310914 24326 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2ccc(F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL134072 24326 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2ccc(F)cc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
10459336 73812 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2N)C1=O 10.1016/j.bmcl.2012.03.007
CHEMBL2018540 73812 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125-I]MCP1 from CCR2 on human PBMCDisplacement of [125-I]MCP1 from CCR2 on human PBMC
ChEMBL 520 10 4 5 3.6 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)N1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2N)C1=O 10.1016/j.bmcl.2012.03.007
44442574 155126 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 517 9 4 5 2.8 Cc1cc(C#N)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL402055 155126 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 517 9 4 5 2.8 Cc1cc(C#N)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
11634118 58450 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 466 5 1 3 5.4 CC(C)[C@]1(C(=O)N2CCC(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
CHEMBL1683053 58450 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2 after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 after 30 mins by gamma counting
ChEMBL 466 5 1 3 5.4 CC(C)[C@]1(C(=O)N2CCC(c3cccc(C(F)(F)F)c3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.015
89823507 126320 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650370 126320 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
56678506 65787 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 545 8 2 9 2.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(S(C)(=O)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834782 65787 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation countingDisplacement of [125I]-MCP1 from human CCR2 receptor in THP1 cells after 2 hrs by scintillation counting
ChEMBL 545 8 2 9 2.2 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(S(C)(=O)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
57401421 67863 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
CHEMBL1910161 67863 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assayDisplacement of [125I]-MIP-1alpha 125I]-MCP1 from CCR2 expressed in CHO ducX#98 cells by scintillation proximity assay
ChEMBL 486 6 1 3 5.1 O=C(NCCCN1CCC(c2ccc(F)cc2)CC1)C1=Cc2cc(Br)ccc2OCC1 10.1016/j.bmcl.2011.09.013
127025445 137460 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
CHEMBL3753719 137460 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 244 2 1 1 3.7 Cc1cccc([C@]2(C)C[C@@H](C)CC=C2C(=O)O)c1 10.1016/j.bmcl.2015.11.051
72663455 129399 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
CHEMBL3671251 129399 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.Binding Assay: THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30° C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 μL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.). Blank values (buffer only) were subtracted from all values and drug treated values were compared to vehicle treated values. 1 μM cold MCP-1 was used for nonspecific binding.
ChEMBL 469 4 1 6 2.3 COC1COCCC1NC1CC2OCCC2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 nan
44416274 158552 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL409162 158552 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in human monocyte cells
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
44425639 86063 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230831 86063 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cellsDisplacement of [125I]MCP1 from mouse CCR2 receptor expressed in CHO cells
ChEMBL 580 6 1 3 6.8 COCC1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CCC(N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11843813 141899 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
CHEMBL386865 141899 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]MCP1 binding to CCR2 expressed in CHO cellsInhibition of [125I]MCP1 binding to CCR2 expressed in CHO cells
ChEMBL 566 8 1 2 7.5 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@H](CCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm060439n
44395079 66995 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 530 8 2 6 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
CHEMBL186899 66995 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cellConcentration required to inhibit [125I]MCP-1 (Monocyte Chemoattractant Protein-1) binding to THP-1 cell
ChEMBL 530 8 2 6 3.9 CS(=O)(=O)c1ccc(CN2CCCN(CCC(O)(c3cccc(O)c3)c3cc(F)cc(F)c3)CC2)cc1 10.1016/j.bmcl.2004.08.008
44439157 91678 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 597 10 2 5 7.8 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.bmcl.2006.10.060
CHEMBL240853 91678 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 minsDisplacement of 125I-hMCP1 from CCR2 expressed in human peripheral blood monocytes after 60 mins
ChEMBL 597 10 2 5 7.8 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.bmcl.2006.10.060
49863168 15204 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 583 9 2 5 7.4 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.ejmech.2010.04.024
CHEMBL1210604 15204 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Inhibition of CCR2Inhibition of CCR2
ChEMBL 583 9 2 5 7.4 O=C(CCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccc2c(n1)NCCC2 10.1016/j.ejmech.2010.04.024
71519227 86375 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 503 4 1 5 3.6 COC1COCCC1N[C@@H]1C[C@H]2CC(F)(F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
CHEMBL2313769 86375 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 503 4 1 5 3.6 COC1COCCC1N[C@@H]1C[C@H]2CC(F)(F)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2012.10.069
11318368 74530 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200199c
CHEMBL2029410 74530 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma countingDisplacement of [125I]MCP1 from human CCR2 in PBMC after 30 mins by gamma counting
ChEMBL 520 7 3 6 2.9 COc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml200199c
89823428 126325 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
CHEMBL3650375 126325 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
72945827 105226 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115102 105226 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 588 5 1 7 3.7 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)Oc3ccccc3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
57391487 130657 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.6 NC(=O)C(N[C@H]1CC[C@H](C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL3681904 130657 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.6 NC(=O)C(N[C@H]1CC[C@H](C2CNc3ccccc32)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
44444100 94032 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 499 6 0 3 6.2 CN(C)c1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
CHEMBL248812 94032 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125]MCP1 from human CCR2 receptor in THP1 cellsDisplacement of [125]MCP1 from human CCR2 receptor in THP1 cells
ChEMBL 499 6 0 3 6.2 CN(C)c1ccc(C2CCN(CC3CCN(C(=O)/C=C/c4ccc(Cl)c(Cl)c4)CC3)CC2)cc1 10.1016/j.bmcl.2007.07.065
44425316 142357 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
CHEMBL388869 142357 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from mouse CCR2 expressed in monocytesDisplacement of [125I]MCP1 from mouse CCR2 expressed in monocytes
ChEMBL 712 9 2 5 8.5 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2csc(NC(=O)c3ccccc3)n2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.10.059
25268442 93948 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 369 6 1 3 3.7 COc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
CHEMBL248358 93948 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cellsDisplacement of [125I]MCP1 from CCR2 receptor expressed in THP1 cells
ChEMBL 369 6 1 3 3.7 COc1cccc(C(=O)Nc2ccc(C[N+](C)(C)C3CCOCC3)cc2)c1 10.1016/j.bmcl.2007.01.115
508870 97474 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 488 6 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270205 97474 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 488 6 3 4 3.7 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2Cl)C1 10.1016/j.bmcl.2008.02.015
22310992 23106 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 363 4 2 3 4.4 O=C(O)c1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
CHEMBL133075 23106 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 363 4 2 3 4.4 O=C(O)c1c(C(=O)O)n(Cc2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2003.10.049
57344301 130644 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCCO3)CC1 nan
CHEMBL3681892 130644 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 540 7 3 4 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc3c(c2)CCCO3)CC1 nan
508742 95574 None 1 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257702 95574 None 1 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
44453538 97928 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272543 97928 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]MCP1 from human CCR2b in THP1 cellsDisplacement of [125I]MCP1 from human CCR2b in THP1 cells
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
72946008 105235 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115111 105235 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 625 7 1 9 1.9 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCCN3CCOCC3)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
10278862 93727 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247206 93727 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 504 10 4 4 3.0 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
22143200 187763 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL495718 187763 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assayDisplacement of radiolabeled MCP1 from CCR2 in human PBMC by millipore filter plate assay
ChEMBL 480 8 4 5 2.8 CSc1ccc(CNC2CCNCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.07.123
9956260 157681 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
CHEMBL408172 157681 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of radiolabeled MCP1 from human CCR2 in PBMCsDisplacement of radiolabeled MCP1 from human CCR2 in PBMCs
ChEMBL 467 7 3 3 4.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@@H]1NCc1ccc(Cl)cc1 10.1021/jm701488f
127025444 137266 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 230 2 1 1 3.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccccc2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752110 137266 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assayDisplacement of [125I]MCP-1 from CCR2 in human PBMC by radioligand displacement assay
ChEMBL 230 2 1 1 3.4 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccccc2)C1 10.1016/j.bmcl.2015.11.051
57656938 75213 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036766 75213 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 410 4 1 3 3.7 O=C(Nc1cccc(C(F)(F)F)c1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
44415922 141681 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
CHEMBL385540 141681 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]MCP-1 from human CCR2b expressed in CHO cellsDisplacement of [125I]MCP-1 from human CCR2b expressed in CHO cells
ChEMBL 536 7 1 2 6.8 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](CCN1CCC2(C=Cc3ccccc32)CC1)C1CC1 10.1016/j.bmcl.2006.07.011
57344318 68931 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922791 68931 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 566 7 2 3 5.6 CN(C)C(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
57344317 68930 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
CHEMBL1922790 68930 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).Binding Assay: MCP-1 Receptor Binding Assay in THP-1 Cells Human monocytic cell line THP-1 cells were obtained from American Type Culture Collection (Manassas, Va., USA). The THP-1 cells were grown in RPMI-1640 (RPMI: Roswell Park Memorial Institute Medium-cell culture growth media) supplemented with 10% fetal bovine serum in a humidified 5% CO2 atmosphere at 37 C. The cell density was maintained between 0.5x106 cells/mL.THP-1 (cells were incubated with 0.5 nM 125I labeled MCP-1 (Perkin-Elmer Life Sciences, Inc. Boston, Mass.) in the presence of varying concentrations of either unlabeled MCP-1 (R & D Systems, Minneapolis, Minn.) or test compound for 2 hours at 30 C. in a 96 well plate. Cells were then harvested onto a filter plate, dried, and 20 uL of Microscint 20 was added to each well. Plates were counted in a TopCount NXT, Microplate Scintillation & Luminescence Counter (Perkin-Elmer Life Sciences, Inc. Boston, Mass.).
ChEMBL 552 7 3 3 5.3 CNC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 nan
72946010 105228 None 0 Human Binding pIC50 = 7 7.0 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
CHEMBL3115104 105228 None 0 Human Binding pIC50 = 7 7.0 - 0
Antagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity at CCR2 receptor in human THP1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 582 5 1 7 3.6 COC1COCCC1N[C@@H]1C[C@H]2CN(C(=O)OCC(C)(C)C)C[C@@]2(C(=O)N2CCc3ncc(C(F)(F)F)cc3C2)C1 10.1016/j.bmcl.2013.05.024
11510932 75200 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036753 75200 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assayDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human THP-1 cell membrane by SPA assay
ChEMBL 460 5 1 3 5.1 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(Cc3ccccc3)C2)CC1 10.1016/j.bmcl.2012.04.118
46886061 7981 None 1 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 6 3.9 CC(C)N(C)[C@@H]1CC[C@H](N2C(=O)C[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090562 7981 None 1 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 minsDisplacement of [125I]-MCP1 from CCR2 in human THP1 cells after 30 mins
ChEMBL 593 8 1 6 3.9 CC(C)N(C)[C@@H]1CC[C@H](N2C(=O)C[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
44442558 93728 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 518 10 4 4 3.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
CHEMBL247207 93728 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125]MCP1 from CCR2 in human PBMCsDisplacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL 518 10 4 4 3.4 Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC2CCCC2)c(C)c1 10.1016/j.bmcl.2007.07.028
22310965 19590 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2c(F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
CHEMBL130008 19590 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human C-C chemokine receptor type 2Inhibition of human C-C chemokine receptor type 2
ChEMBL 337 3 1 2 4.8 O=C(O)c1cc2c(F)cccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2003.10.049
46885027 8419 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8419 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cellsDisplacement of [125I]MCP1 from human CCR2B receptor expressed in HEK293-EBNA cells
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
10343454 3981 None 29 Human Binding pKd = 10 10.0 34 2
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
9046 3981 None 29 Human Binding pKd = 10 10.0 34 2
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
CHEMBL2178578 3981 None 29 Human Binding pKd = 10 10.0 34 2
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
DB15250 3981 None 29 Human Binding pKd = 10 10.0 34 2
Binding affinity to CCR2 (unknown origin) assessed as dissociation constantBinding affinity to CCR2 (unknown origin) assessed as dissociation constant
ChEMBL 444 5 1 4 4.3 Clc1ccc(c(c1)C(=O)c1cc[n+](cc1)[O-])NS(=O)(=O)c1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.6b01309
11180808 2547 None 52 Human Binding pKd = 9.3 9.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
9048 2547 None 52 Human Binding pKd = 9.3 9.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
CHEMBL3305901 2547 None 52 Human Binding pKd = 9.3 9.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
155491018 174081 None 1 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
53389902 172497 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4483373 172497 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155491018 174081 None 1 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174081 None 1 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
53389902 172497 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4483373 172497 None 0 Human Binding pKi = 9.4 9.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.8 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)c(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
11180808 2547 None 52 Human Binding pKi = 9.3 9.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
9048 2547 None 52 Human Binding pKi = 9.3 9.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
CHEMBL3305901 2547 None 52 Human Binding pKi = 9.3 9.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 469 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F 10.1016/j.ejmech.2015.01.063
71717723 87827 None 0 Human Binding pKi = 9.2 9.2 51 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 525 7 2 7 4.3 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(CF)nc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1021/ml400055e
CHEMBL2338392 87827 None 0 Human Binding pKi = 9.2 9.2 51 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 525 7 2 7 4.3 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(CF)nc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1021/ml400055e
155554273 174211 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4548396 174211 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
155554273 174211 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4548396 174211 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 182272 None 1 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162666730 182272 None 1 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155554106 175467 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4577171 175467 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155562719 175227 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4571719 175227 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155562719 175227 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4571719 175227 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 407 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(I)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155554106 175467 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4577171 175467 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Br)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
71718331 87826 None 0 Human Binding pKi = 9 9.0 208 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 663 8 2 8 5.7 Cc1c(NC[C@H]2CCC[C@@H](c3ccc(C(F)(F)F)cc3)O2)nc(C2CCOCC2)nc1C(=O)N1CCC(N[C@H]2CCOC[C@H]2F)CC1 10.1021/ml400055e
CHEMBL2338391 87826 None 0 Human Binding pKi = 9 9.0 208 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 663 8 2 8 5.7 Cc1c(NC[C@H]2CCC[C@@H](c3ccc(C(F)(F)F)cc3)O2)nc(C2CCOCC2)nc1C(=O)N1CCC(N[C@H]2CCOC[C@H]2F)CC1 10.1021/ml400055e
71719547 87828 None 0 Human Binding pKi = 9 9.0 50 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 660 8 2 9 5.8 Cc1cc(-c2nc(NC[C@H]3CCC[C@@H](c4ccc(C(F)(F)F)cc4)O3)c(C)c(C(=O)N3CCC(N[C@@H]4CCOC[C@@H]4F)CC3)n2)no1 10.1021/ml400055e
CHEMBL2338393 87828 None 0 Human Binding pKi = 9 9.0 50 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 660 8 2 9 5.8 Cc1cc(-c2nc(NC[C@H]3CCC[C@@H](c4ccc(C(F)(F)F)cc4)O3)c(C)c(C(=O)N3CCC(N[C@@H]4CCOC[C@@H]4F)CC3)n2)no1 10.1021/ml400055e
118734584 118694 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1cc2c(cc1OC)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
CHEMBL3417124 118694 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1cc2c(cc1OC)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
53389845 172959 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172959 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389845 172959 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172959 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155563012 175279 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4572833 175279 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155563012 175279 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4572833 175279 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 3 2 5 2.2 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Br)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10585 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155513284 169724 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4438407 169724 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
118734578 118687 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Cl)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417117 118687 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Cl)ccc32)C1 10.1016/j.ejmech.2015.01.063
10585 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155513284 169724 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4438407 169724 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 343 3 2 5 2.9 Nc1nc2[nH]c(C3CCCC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389660 171481 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 171481 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
53389660 171481 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 171481 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
155553917 174201 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4548107 174201 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155553917 174201 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4548107 174201 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(Cl)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389637 170565 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4450273 170565 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
53389637 170565 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4450273 170565 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 3 2 5 2.4 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 182272 None 1 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
15985912 83973 None 0 Human Binding pKi = 8 8.0 2 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83973 None 0 Human Binding pKi = 8 8.0 2 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461438 83974 None 0 Human Binding pKi = 8 8.0 100 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207082 83974 None 0 Human Binding pKi = 8 8.0 100 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214709 83976 None 0 Human Binding pKi = 8 8.0 14 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207084 83976 None 0 Human Binding pKi = 8 8.0 14 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.8 Cc1nnnn1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71450658 83990 None 0 Human Binding pKi = 8 8.0 15 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207098 83990 None 0 Human Binding pKi = 8 8.0 15 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
15985912 83973 None 0 Human Binding pKi = 8 8.0 2 3
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83973 None 0 Human Binding pKi = 8 8.0 2 3
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
118734680 118702 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 547 5 1 3 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccnc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417225 118702 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 547 5 1 3 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccnc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734682 118704 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 591 7 1 4 7.5 CCOc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417227 118704 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 591 7 1 4 7.5 CCOc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
12093167 172323 None 33 Human Binding pKi = 8 8.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 172323 None 33 Human Binding pKi = 8 8.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823581 126359 None 0 Human Binding pKi = 8 8.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650407 126359 None 0 Human Binding pKi = 8 8.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
10436045 3514 None 4 Human Binding pKi = 7 7.0 -85 13
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 7 7.0 -85 13
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 7 7.0 -85 13
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3514 None 4 Human Binding pKi = 7 7.0 -85 13
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
782 3514 None 4 Human Binding pKi = 7 7.0 -85 13
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
CHEMBL432713 3514 None 4 Human Binding pKi = 7 7.0 -85 13
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01309
71461439 83979 None 0 Human Binding pKi = 7 7.0 10 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207087 83979 None 0 Human Binding pKi = 7 7.0 10 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
71452487 83980 None 0 Human Binding pKi = 7 7.0 12 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207088 83980 None 0 Human Binding pKi = 7 7.0 12 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
71454247 83982 None 0 Human Binding pKi = 7 7.0 15 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207090 83982 None 0 Human Binding pKi = 7 7.0 15 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 366 5 1 5 2.9 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(F)c1 10.1016/j.bmcl.2012.09.020
155539148 172802 None 0 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172802 None 0 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155539148 172802 None 0 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4513770 172802 None 0 Human Binding pKi = 7.0 7.0 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 4.1 CCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823497 126300 None 0 Human Binding pKi = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650350 126300 None 0 Human Binding pKi = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
155536512 172203 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4473756 172203 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
3013430 21129 None 1 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
183790 3740 None 11 Human Binding pKi = 7.0 7.0 -6 2
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 7.0 7.0 -6 2
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 7.0 7.0 -6 2
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155536512 172203 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4473756 172203 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
89823576 126327 None 0 Human Binding pKi = 6.0 6.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
CHEMBL3650377 126327 None 0 Human Binding pKi = 6.0 6.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 542 5 1 6 3.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ncc(C(F)(F)F)cc2Cl)C1 nan
89823413 126331 None 0 Human Binding pKi = 6.0 6.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
CHEMBL3650381 126331 None 0 Human Binding pKi = 6.0 6.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C#N)ccc2C(F)(F)F)C1 nan
118734676 118699 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4ccc(C#N)cc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417221 118699 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4ccc(C#N)cc4)ccc32)C1 10.1016/j.ejmech.2015.01.063
12093167 172323 None 33 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4475389 172323 None 33 Human Binding pKi = 8.0 8.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 351 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823461 126315 None 0 Human Binding pKi = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
CHEMBL3650365 126315 None 0 Human Binding pKi = 7.0 7.0 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 491 5 1 5 3.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(Cl)c2)C1 nan
118734684 118706 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 595 6 1 4 7.3 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c(F)cn1 10.1016/j.ejmech.2015.01.063
CHEMBL3417229 118706 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 595 6 1 4 7.3 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c(F)cn1 10.1016/j.ejmech.2015.01.063
71745103 126360 None 0 Human Binding pKi = 7.9 7.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650408 126360 None 0 Human Binding pKi = 7.9 7.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3740 None 11 Human Binding pKi = 7.9 7.9 -6 2
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 7.9 7.9 -6 2
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 7.9 7.9 -6 2
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
71454248 83993 None 0 Human Binding pKi = 7.9 7.9 25 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207100 83993 None 0 Human Binding pKi = 7.9 7.9 25 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
71214976 83994 None 0 Human Binding pKi = 7.9 7.9 79 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207101 83994 None 0 Human Binding pKi = 7.9 7.9 79 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
155545321 173452 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4529401 173452 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
89823621 126317 None 0 Human Binding pKi = 6.9 6.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
CHEMBL3650367 126317 None 0 Human Binding pKi = 6.9 6.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)n2)C1 nan
71463165 83978 None 0 Human Binding pKi = 5.9 5.9 6 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207086 83978 None 0 Human Binding pKi = 5.9 5.9 6 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 348 5 1 5 2.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccccc1 10.1016/j.bmcl.2012.09.020
9870980 154645 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL399472 154645 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 509 6 2 2 7.0 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccccc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
25110660 154870 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154870 None 0 Human Binding pKi = 6.9 6.9 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
10436045 3514 None 4 Human Binding pKi = 6.9 6.9 -85 13
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 6.9 6.9 -85 13
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 6.9 6.9 -85 13
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118734580 118690 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 538 4 1 2 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(C(F)(F)F)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417120 118690 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 538 4 1 2 7.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(C(F)(F)F)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734582 118692 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(C#N)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417122 118692 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(C#N)cc32)C1 10.1016/j.ejmech.2015.01.063
118734688 118710 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 592 5 1 3 7.4 COc1cc2c(cc1Br)C(C)CC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417233 118710 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 592 5 1 3 7.4 COc1cc2c(cc1Br)C(C)CC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
155545321 173452 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4529401 173452 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
89823598 126363 None 0 Human Binding pKi = 7.9 7.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650410 126363 None 0 Human Binding pKi = 7.9 7.9 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3740 None 11 Human Binding pKi = 5.9 5.9 -6 2
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 5.9 5.9 -6 2
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 5.9 5.9 -6 2
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118734694 118717 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417240 118717 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
9902578 171353 None 0 Human Binding pKi = 6.9 6.9 -4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 171353 None 0 Human Binding pKi = 6.9 6.9 -4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
118723411 116322 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 503 6 3 4 4.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3359300 116322 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 503 6 3 4 4.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc(O)cc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
155523645 170876 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4454297 170876 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155523645 170876 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4454297 170876 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3Cl)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
9902578 171353 None 0 Human Binding pKi = 6.8 6.8 -4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4461627 171353 None 0 Human Binding pKi = 6.8 6.8 -4 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 5 1 3 4.5 CCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3740 None 11 Human Binding pKi = 6.8 6.8 -6 2
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 6.8 6.8 -6 2
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 6.8 6.8 -6 2
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
54597147 161370 None 0 Human Binding pKi = 7.8 7.8 - 1
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 594 5 0 7 3.3 Cc1c(C(=O)N2CCC(N3CCC(N(C)S(C)(=O)=O)CC3)CC2)ncnc1N1CCc2ccc(C(F)(F)F)cc2C1 10.1016/j.bmc.2018.05.027
CHEMBL4126162 161370 None 0 Human Binding pKi = 7.8 7.8 - 1
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 594 5 0 7 3.3 Cc1c(C(=O)N2CCC(N3CCC(N(C)S(C)(=O)=O)CC3)CC2)ncnc1N1CCc2ccc(C(F)(F)F)cc2C1 10.1016/j.bmc.2018.05.027
118734571 118680 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 500 5 1 4 5.2 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417110 118680 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 500 5 1 4 5.2 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
118734575 118684 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(C#N)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417114 118684 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 495 4 1 3 5.9 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(C#N)cccc32)C1 10.1016/j.ejmech.2015.01.063
155521447 170582 None 0 Human Binding pKi = 7.8 7.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170582 None 0 Human Binding pKi = 7.8 7.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
89823526 126345 None 0 Human Binding pKi = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650394 126345 None 0 Human Binding pKi = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 538 4 0 4 5.7 O=C(N1C[C@@H]2C[C@H]1CN2c1cc(C(F)(F)F)ccn1)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
155521447 170582 None 0 Human Binding pKi = 7.8 7.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
CHEMBL4450561 170582 None 0 Human Binding pKi = 7.8 7.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 421 4 1 3 4.7 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)C1CC1 10.1021/acs.jmedchem.8b00605
155518928 170343 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4447263 170343 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
155518928 170343 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
CHEMBL4447263 170343 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccccc1Cc1c(C2CC2)[nH]c2nc(N)nn2c1=O 10.1021/acs.jmedchem.9b00742
12093170 871 None 31 Human Binding pKi = 7.8 7.8 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
9431 871 None 31 Human Binding pKi = 7.8 7.8 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL4519152 871 None 31 Human Binding pKi = 7.8 7.8 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C 10.1021/acs.jmedchem.6b01309
CHEMBL5268600 193570 None 0 Human Binding pKi = 7.8 7.8 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 577 8 3 7 3.2 CCO[C@H]1CN(C2CCC(O)(c3ccc4c(c3)OCO4)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1021/acs.jmedchem.6b01309
71214710 83977 None 0 Human Binding pKi = 7.8 7.8 39 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207085 83977 None 0 Human Binding pKi = 7.8 7.8 39 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
10293022 171096 None 12 Human Binding pKi = 7.8 7.8 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 171096 None 12 Human Binding pKi = 7.8 7.8 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
3013430 21129 None 1 Human Binding pKi = 6.8 6.8 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 6.8 6.8 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155530253 171519 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4464168 171519 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
155545804 173495 None 0 Human Binding pKi = 6.8 6.8 -5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 173495 None 0 Human Binding pKi = 6.8 6.8 -5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10132885 175136 None 0 Human Binding pKi = 6.8 6.8 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 175136 None 0 Human Binding pKi = 6.8 6.8 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155545804 173495 None 0 Human Binding pKi = 6.8 6.8 -5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4530510 173495 None 0 Human Binding pKi = 6.8 6.8 -5 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 6 1 3 4.9 CCCCC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10132885 175136 None 0 Human Binding pKi = 6.8 6.8 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4569870 175136 None 0 Human Binding pKi = 6.8 6.8 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 355 3 1 3 4.7 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155535265 172017 None 0 Human Binding pKi = 6.8 6.8 -8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 172017 None 0 Human Binding pKi = 6.8 6.8 -8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155530253 171519 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4464168 171519 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 365 3 2 5 3.2 Cc1ccc(-c2[nH]c3nc(N)nn3c(=O)c2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b00742
71456007 83984 None 0 Human Binding pKi = 5.8 5.8 1 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207092 83984 None 0 Human Binding pKi = 5.8 5.8 1 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
89823445 126349 None 0 Human Binding pKi = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650398 126349 None 0 Human Binding pKi = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
10436045 3514 None 4 Human Binding pKi = 7.8 7.8 -85 13
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 7.8 7.8 -85 13
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 7.8 7.8 -85 13
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
53389980 172225 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474089 172225 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155535265 172017 None 0 Human Binding pKi = 6.8 6.8 -8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4471583 172017 None 0 Human Binding pKi = 6.8 6.8 -8 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 339 4 1 3 4.1 Cc1ccc(N2C(=O)C(O)=C(C(=O)C3CC3)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
5353432 97493 None 89 Human Binding pKi = 5.8 5.8 -1 3
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97493 None 89 Human Binding pKi = 5.8 5.8 -1 3
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
9924108 171771 None 0 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171771 None 0 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
10436045 3514 None 4 Human Binding pKi = 6.8 6.8 -85 13
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 6.8 6.8 -85 13
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 6.8 6.8 -85 13
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3514 None 4 Human Binding pKi = 6.8 6.8 -85 13
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 6.8 6.8 -85 13
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 6.8 6.8 -85 13
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10293022 171096 None 12 Human Binding pKi = 7.8 7.8 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4457687 171096 None 12 Human Binding pKi = 7.8 7.8 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 377 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823661 126342 None 0 Human Binding pKi = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650391 126342 None 0 Human Binding pKi = 7.8 7.8 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 541 5 1 5 4.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
53389980 172225 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474089 172225 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 289 2 2 5 1.6 Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
183790 3740 None 11 Human Binding pKi = 7.8 7.8 -6 2
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 7.8 7.8 -6 2
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 7.8 7.8 -6 2
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
22335694 171556 None 0 Human Binding pKi = 7.8 7.8 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 171556 None 0 Human Binding pKi = 7.8 7.8 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9924108 171771 None 0 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4467708 171771 None 0 Human Binding pKi = 6.8 6.8 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.5 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCCC1 10.1021/acs.jmedchem.8b00605
781 3394 None 80 Human Binding pKi = 6.8 6.8 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 6.8 6.8 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 6.8 6.8 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
155522874 170837 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4453718 170837 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155522874 170837 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4453718 170837 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 373 8 2 5 3.8 CCCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
22335694 171556 None 0 Human Binding pKi = 7.8 7.8 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4464639 171556 None 0 Human Binding pKi = 7.8 7.8 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9902204 170124 None 12 Human Binding pKi = 7.7 7.7 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 170124 None 12 Human Binding pKi = 7.7 7.7 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3740 None 11 Human Binding pKi = 6.7 6.7 -6 2
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 6.7 6.7 -6 2
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 6.7 6.7 -6 2
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
44353447 3773 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
9902204 170124 None 12 Human Binding pKi = 7.7 7.7 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4443909 170124 None 12 Human Binding pKi = 7.7 7.7 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
162671727 182969 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4793148 182969 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
118734693 118716 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417239 118716 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
89823498 126311 None 0 Human Binding pKi = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
CHEMBL3650361 126311 None 0 Human Binding pKi = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C)C1 nan
781 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
9953769 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
CHEMBL134074 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/acs.jmedchem.6b01309
3794409 170754 None 7 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170754 None 7 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
76167595 161462 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 493 6 2 7 3.8 COC1COCCC1NC1CCN(C(=O)c2ncnc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127538 161462 None 0 Human Binding pKi = 8.7 8.7 - 1
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 493 6 2 7 3.8 COC1COCCC1NC1CCN(C(=O)c2ncnc(Nc3ccc(Cl)c(Cl)c3)c2C)CC1 10.1016/j.bmc.2018.05.027
118734686 118708 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccc(Br)cc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417231 118708 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccc(Br)cc21 10.1016/j.ejmech.2015.01.063
118734691 118714 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417237 118714 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
183790 3740 None 11 Human Binding pKi = 8.7 8.7 -6 2
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3740 None 11 Human Binding pKi = 8.7 8.7 -6 2
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3740 None 11 Human Binding pKi = 8.7 8.7 -6 2
Displacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometryDisplacement of [125I]-CCL2 from human CCR2 expressed in U2OS cells incubated for 150 mins by scintillation spectrometry
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
71718930 87825 None 0 Human Binding pKi = 8.7 8.7 75 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 601 5 1 7 4.4 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(C(F)(F)F)nc(N3CCc4cc(C(F)(F)F)ccc4C3)c2C)CC1 10.1021/ml400055e
CHEMBL2338390 87825 None 0 Human Binding pKi = 8.7 8.7 75 2
Displacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysisDisplacement of [125I]MCP1 from CCR2 in human THP1 cell membranes after 8 hrs by scintillation counting analysis
ChEMBL 601 5 1 7 4.4 CO[C@@H]1COCC[C@@H]1NC1CCN(C(=O)c2nc(C(F)(F)F)nc(N3CCc4cc(C(F)(F)F)ccc4C3)c2C)CC1 10.1021/ml400055e
155551912 175134 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4569807 175134 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
155551912 175134 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4569807 175134 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 439 3 2 5 3.2 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Br)cc(Br)c1 10.1021/acs.jmedchem.9b00742
155540798 172933 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4516788 172933 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
118734572 118681 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 470 4 1 2 6.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417111 118681 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 470 4 1 2 6.1 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
155540798 172933 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4516788 172933 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)cc(Cl)c1 10.1021/acs.jmedchem.9b00742
53389710 172279 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474757 172279 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
71576618 118688 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417118 118688 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
53389710 172279 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4474757 172279 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 331 5 2 5 2.6 CCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
73334813 118712 None 17 Human Binding pKi = 8.6 8.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417235 118712 None 17 Human Binding pKi = 8.6 8.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
162666730 182272 None 1 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155560784 175049 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4567816 175049 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
155560784 175049 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4567816 175049 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1cccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)c1 10.1021/acs.jmedchem.9b00742
183790 3740 None 11 Human Binding pKi = 8.6 8.6 -6 2
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 8.6 8.6 -6 2
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 8.6 8.6 -6 2
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155541801 173054 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4519409 173054 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155527193 171167 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4458846 171167 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
155527193 171167 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4458846 171167 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 311 4 2 6 1.5 COc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
3013430 21129 None 1 Human Binding pKi = 5.7 5.7 - 1
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 5.7 5.7 - 1
Binding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards E291Q receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
3794409 170754 None 7 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4452558 170754 None 7 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.8b00605
89823496 126313 None 0 Human Binding pKi = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
CHEMBL3650363 126313 None 0 Human Binding pKi = 6.7 6.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 3.8 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(C(F)(F)F)c2)C1 nan
781 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10436045 3514 None 4 Human Binding pKi = 5.7 5.7 -85 13
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 5.7 5.7 -85 13
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 5.7 5.7 -85 13
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118734576 118685 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 486 4 2 3 5.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(O)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417115 118685 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 486 4 2 3 5.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(O)cccc32)C1 10.1016/j.ejmech.2015.01.063
89823628 126347 None 0 Human Binding pKi = 7.7 7.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
CHEMBL3650396 126347 None 0 Human Binding pKi = 7.7 7.7 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 555 5 0 5 4.8 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C(F)(F)F)c2)C1 nan
183790 3740 None 11 Human Binding pKi = 7.7 7.7 -6 2
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 7.7 7.7 -6 2
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 7.7 7.7 -6 2
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
155550777 174285 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4549837 174285 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
3796276 170848 None 7 Human Binding pKi = 6.7 6.7 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170848 None 7 Human Binding pKi = 6.7 6.7 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
155526680 171127 None 0 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 171127 None 0 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
12093162 173324 None 0 Human Binding pKi = 6.7 6.7 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 173324 None 0 Human Binding pKi = 6.7 6.7 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
3796276 170848 None 7 Human Binding pKi = 6.7 6.7 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4453953 170848 None 7 Human Binding pKi = 6.7 6.7 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 385 3 1 3 4.2 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1c1ccc(Br)cc1 10.1021/acs.jmedchem.8b00605
155526680 171127 None 0 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
CHEMBL4458295 171127 None 0 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 467 3 1 3 4.8 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1c1cccc(Br)c1 10.1021/acs.jmedchem.8b00605
12093162 173324 None 0 Human Binding pKi = 6.7 6.7 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4526524 173324 None 0 Human Binding pKi = 6.7 6.7 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 329 4 1 4 3.4 COc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
781 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 6.7 6.7 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
162671727 182969 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4793148 182969 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 601 10 3 5 5.6 C=CC(=O)NCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155550777 174285 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4549837 174285 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 7 2 5 3.4 CCCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155513605 169778 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
CHEMBL4439033 169778 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
155513605 169778 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
CHEMBL4439033 169778 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 3.0 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1cc(Cl)ccc1Cl 10.1021/acs.jmedchem.9b00742
155553131 174109 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4545333 174109 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10436045 3514 None 4 Human Binding pKi = 6.6 6.6 -85 13
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 6.6 6.6 -85 13
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 6.6 6.6 -85 13
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
3013430 21129 None 1 Human Binding pKi = 6.6 6.6 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 6.6 6.6 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
118734581 118691 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1ccc2c(c1)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
CHEMBL3417121 118691 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1ccc2c(c1)C(N[C@@H]1CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C1)CC2 10.1016/j.ejmech.2015.01.063
118734683 118705 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)ccn1 10.1016/j.ejmech.2015.01.063
CHEMBL3417228 118705 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)ccn1 10.1016/j.ejmech.2015.01.063
3013430 21129 None 1 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
9967465 172085 None 11 Human Binding pKi = 6.6 6.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 172085 None 11 Human Binding pKi = 6.6 6.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9967465 172085 None 11 Human Binding pKi = 6.6 6.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4472384 172085 None 11 Human Binding pKi = 6.6 6.6 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 333 3 1 3 4.0 CC(=O)C1=C(O)C(=O)N(c2cccc(Cl)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
68070944 161458 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 582 8 1 7 4.1 CCS(=O)(=O)N(C)C1CCN(C2CCN(C(=O)c3ncnc(NCc4ccc(Cl)c(Cl)c4)c3C)CC2)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127496 161458 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to human CCR2Binding affinity to human CCR2
ChEMBL 582 8 1 7 4.1 CCS(=O)(=O)N(C)C1CCN(C2CCN(C(=O)c3ncnc(NCc4ccc(Cl)c(Cl)c4)c3C)CC2)CC1 10.1016/j.bmc.2018.05.027
118734690 118713 None 3 Human Binding pKi = 7.6 7.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417236 118713 None 3 Human Binding pKi = 7.6 7.6 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 548 4 1 2 6.8 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2CCc3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
10436045 3514 None 4 Human Binding pKi = 5.6 5.6 -85 13
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 5.6 5.6 -85 13
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 5.6 5.6 -85 13
Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
71450657 83986 None 0 Human Binding pKi = 7.6 7.6 15 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207094 83986 None 0 Human Binding pKi = 7.6 7.6 15 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
15604497 83991 None 0 Human Binding pKi = 7.6 7.6 39 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207099 83991 None 0 Human Binding pKi = 7.6 7.6 39 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
44309012 102821 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102821 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
71463166 83988 None 0 Human Binding pKi = 6.6 6.6 7 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207096 83988 None 0 Human Binding pKi = 6.6 6.6 7 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 390 5 1 8 2.3 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc2nonc12 10.1016/j.bmcl.2012.09.020
44309012 102821 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102821 None 0 Human Binding pKi = 6.6 6.6 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
781 3394 None 80 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
10436045 3514 None 4 Human Binding pKi = 5.6 5.6 -85 13
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 5.6 5.6 -85 13
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 5.6 5.6 -85 13
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
44353447 3773 None 0 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
3013430 21129 None 1 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 5.6 5.6 - 1
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
11080 29083 None 79 Human Binding pKi = 5.6 5.6 -1 6
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 29083 None 79 Human Binding pKi = 5.6 5.6 -1 6
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
155553131 174109 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4545333 174109 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 351 3 2 5 2.9 Nc1nc2[nH]c(-c3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
89823470 126307 None 0 Human Binding pKi = 6.6 6.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
CHEMBL3650357 126307 None 0 Human Binding pKi = 6.6 6.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nccc(C(F)(F)F)n2)C1 nan
12093163 174400 None 0 Human Binding pKi = 6.6 6.6 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 174400 None 0 Human Binding pKi = 6.6 6.6 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
12093163 174400 None 0 Human Binding pKi = 6.6 6.6 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4552420 174400 None 0 Human Binding pKi = 6.6 6.6 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2cccc(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3740 None 11 Human Binding pKi = 7.6 7.6 -6 2
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 7.6 7.6 -6 2
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 7.6 7.6 -6 2
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118723406 116320 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 501 6 2 3 5.1 Cc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
CHEMBL3359295 116320 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 501 6 2 3 5.1 Cc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
89823507 126320 None 0 Human Binding pKi = 6.6 6.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
CHEMBL3650370 126320 None 0 Human Binding pKi = 6.6 6.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(F)cc(C(F)(F)F)c2)C1 nan
89823552 126301 None 0 Human Binding pKi = 7.6 7.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
CHEMBL3650351 126301 None 0 Human Binding pKi = 7.6 7.6 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)cnn2)C1 nan
183790 3740 None 11 Human Binding pKi = 7.5 7.5 -6 2
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 7.5 7.5 -6 2
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 7.5 7.5 -6 2
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
3013430 21129 None 1 Human Binding pKi = 7.5 7.5 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 7.5 7.5 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
44353447 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
155540563 172535 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483756 172535 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9949615 138202 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 335 3 2 3 4.4 O=C(O)c1cc2cc(O)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2006.04.045
CHEMBL376981 138202 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 335 3 2 3 4.4 O=C(O)c1cc2cc(O)ccc2n1Cc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2006.04.045
89823551 126310 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
CHEMBL3650360 126310 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(F)c(C(F)(F)F)c2)C1 nan
118734685 118707 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.6 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccccc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417230 118707 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.6 CC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2ccccc21 10.1016/j.ejmech.2015.01.063
155541801 173054 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4519409 173054 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155535293 172043 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4471792 172043 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
53389636 172398 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4476551 172398 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155543260 173287 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4525646 173287 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155535293 172043 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
CHEMBL4471792 172043 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 295 3 2 5 1.8 Cc1ccc(Cc2c(C3CC3)[nH]c3nc(N)nn3c2=O)cc1 10.1021/acs.jmedchem.9b00742
155543260 173287 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4525646 173287 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 314 3 1 4 2.8 Cc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
53389636 172398 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4476551 172398 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 317 4 2 5 2.2 CCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
162666730 182272 None 1 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 181094 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
53389641 175951 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4588111 175951 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
86698129 126302 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650352 126302 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 522 5 0 6 3.6 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
3013430 21129 None 1 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155540563 172535 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483756 172535 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2cccc(C(F)(F)F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823349 126314 None 0 Human Binding pKi = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
CHEMBL3650364 126314 None 0 Human Binding pKi = 6.5 6.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 521 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C)c(C(F)(F)F)c2)C1 nan
118734573 118682 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1cccc2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417112 118682 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 484 4 1 2 6.4 Cc1cccc2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
162671079 182850 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4791522 182850 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
89823575 126309 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
CHEMBL3650359 126309 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 525 5 1 5 4.0 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2F)C1 nan
15985914 83972 None 0 Human Binding pKi = 7.5 7.5 8 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207080 83972 None 0 Human Binding pKi = 7.5 7.5 8 2
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 457 6 1 6 4.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1nnnc1C1CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461440 83989 None 0 Human Binding pKi = 7.5 7.5 31 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207097 83989 None 0 Human Binding pKi = 7.5 7.5 31 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
162671079 182850 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4791522 182850 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.4 O=C(NCCN=C=S)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
155513751 169799 None 0 Human Binding pKi = 6.5 6.5 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169799 None 0 Human Binding pKi = 6.5 6.5 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
44353447 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
44353447 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
44353447 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
785 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
CHEMBL337246 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/acs.jmedchem.6b01309
155513751 169799 None 0 Human Binding pKi = 6.5 6.5 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4439354 169799 None 0 Human Binding pKi = 6.5 6.5 -7 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 341 4 1 3 4.3 Cc1ccc(N2C(=O)C(O)=C(C(=O)C(C)C)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
89823537 126296 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650346 126296 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
89823606 126323 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
CHEMBL3650373 126323 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C#N)C1 nan
89823656 126353 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650401 126353 None 0 Human Binding pKi = 7.5 7.5 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 546 5 0 6 4.1 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
44353447 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
9967349 173063 None 0 Human Binding pKi = 7.4 7.4 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 173063 None 0 Human Binding pKi = 7.4 7.4 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9967349 173063 None 0 Human Binding pKi = 7.4 7.4 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4519533 173063 None 0 Human Binding pKi = 7.4 7.4 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823580 126335 None 0 Human Binding pKi = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
CHEMBL3650385 126335 None 0 Human Binding pKi = 7.4 7.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 507 5 1 5 4.1 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(Cl)c2)C1 nan
118734678 118700 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1cccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417223 118700 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1cccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
71214725 83975 None 0 Human Binding pKi = 7.4 7.4 15 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207083 83975 None 0 Human Binding pKi = 7.4 7.4 15 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
10257042 204359 None 0 Human Binding pKi = 7.4 7.4 12 7
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 204359 None 0 Human Binding pKi = 7.4 7.4 12 7
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
162666730 182272 None 1 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4783861 182272 None 1 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 589 9 2 6 6.5 N#CSCCNC(=O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
53389641 175951 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4588111 175951 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 303 3 2 5 1.8 CCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155520385 170448 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4448714 170448 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155520385 170448 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4448714 170448 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 299 3 2 5 1.6 Nc1nc2[nH]c(C3CC3)c(Cc3ccc(F)cc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
183790 3740 None 11 Human Binding pKi = 8.4 8.4 -6 2
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 8.4 8.4 -6 2
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 8.4 8.4 -6 2
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118734579 118689 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 596 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(I)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417119 118689 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 596 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(I)ccc32)C1 10.1016/j.ejmech.2015.01.063
162658125 181094 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 0 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
118734687 118709 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 578 5 1 3 6.8 COc1cc2c(cc1Br)CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417232 118709 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 578 5 1 3 6.8 COc1cc2c(cc1Br)CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
118734574 118683 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 485 4 2 3 5.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(N)cccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417113 118683 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 485 4 2 3 5.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3c(N)cccc32)C1 10.1016/j.ejmech.2015.01.063
118734692 118715 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417238 118715 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 562 4 1 2 7.4 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](N[C@H]2C[C@H](C)c3cc(Br)ccc32)C1 10.1016/j.ejmech.2015.01.063
118734577 118686 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 488 4 1 2 6.2 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(F)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417116 118686 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 488 4 1 2 6.2 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(F)ccc32)C1 10.1016/j.ejmech.2015.01.063
10257042 204359 None 0 Human Binding pKi = 7.4 7.4 12 7
Binding affinity for C-C chemokine receptor type 2B was determinedBinding affinity for C-C chemokine receptor type 2B was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 204359 None 0 Human Binding pKi = 7.4 7.4 12 7
Binding affinity for C-C chemokine receptor type 2B was determinedBinding affinity for C-C chemokine receptor type 2B was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
11632418 75195 None 1 Human Binding pKi = 6.4 6.4 - 1
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membraneDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membrane
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036748 75195 None 1 Human Binding pKi = 6.4 6.4 - 1
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membraneDisplacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membrane
ChEMBL 384 3 1 3 3.5 CN1CCCC(CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
118734681 118703 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
CHEMBL3417226 118703 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 577 6 1 4 7.1 COc1cncc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c1 10.1016/j.ejmech.2015.01.063
176 398 None 66 Human Binding pKi = 5.4 5.4 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 66 Human Binding pKi = 5.4 5.4 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 66 Human Binding pKi = 5.4 5.4 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 66 Human Binding pKi = 5.4 5.4 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 66 Human Binding pKi = 5.4 5.4 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
89823586 126322 None 0 Human Binding pKi = 6.4 6.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
CHEMBL3650372 126322 None 0 Human Binding pKi = 6.4 6.4 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)n2)C1 nan
781 3394 None 80 Human Binding pKi = 6.4 6.4 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 6.4 6.4 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 6.4 6.4 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
89823444 126324 None 0 Human Binding pKi = 6.3 6.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
CHEMBL3650374 126324 None 0 Human Binding pKi = 6.3 6.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 523 6 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cccc(OC(F)(F)F)c2)C1 nan
3013430 21129 None 1 Human Binding pKi = 5.3 5.3 - 1
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 5.3 5.3 - 1
Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
118734671 118697 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1ccc(OC)c2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417216 118697 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 530 6 1 4 6.1 COc1ccc(OC)c2c1CCC2N[C@@H]1CC[C@@](C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)(C(C)C)C1 10.1016/j.ejmech.2015.01.063
89823344 126348 None 0 Human Binding pKi = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650397 126348 None 0 Human Binding pKi = 7.3 7.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 589 5 0 5 5.2 CO[C@@H]1COCC[C@@H]1N(C)[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
155534565 171969 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4470785 171969 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155529754 171459 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4463383 171459 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10111333 175465 None 0 Human Binding pKi = 8.3 8.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175465 None 0 Human Binding pKi = 8.3 8.3 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
155529754 171459 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4463383 171459 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 349 3 2 5 2.5 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(C(F)(F)F)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155534565 171969 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4470785 171969 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 281 3 2 5 1.5 Nc1nc2[nH]c(C3CC3)c(Cc3ccccc3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
10436045 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Binding affinity at C-C chemokine receptor type 2 was determinedBinding affinity at C-C chemokine receptor type 2 was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
44573568 187468 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL494019 187468 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 512 6 2 2 6.8 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCc3ccccc32)C1 10.1016/j.ejmech.2015.01.063
10436045 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
782 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
CHEMBL432713 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Displacement of [125I]MCP1 from human CCR2 expressed in CHO cellsDisplacement of [125I]MCP1 from human CCR2 expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.04.045
10436045 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
71457815 83983 None 0 Human Binding pKi = 7.3 7.3 19 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207091 83983 None 0 Human Binding pKi = 7.3 7.3 19 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
71452488 83985 None 0 Human Binding pKi = 7.3 7.3 19 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207093 83985 None 0 Human Binding pKi = 7.3 7.3 19 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
10436045 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2)
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
10436045 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3514 None 4 Human Binding pKi = 7.3 7.3 -85 13
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
15985981 83971 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 443 5 1 4 5.0 Cc1cc(C)n(Cc2ccc(C(F)(F)F)cc2NS(=O)(=O)c2ccc(Cl)cc2)n1 10.1016/j.bmcl.2012.09.020
CHEMBL2207079 83971 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 443 5 1 4 5.0 Cc1cc(C)n(Cc2ccc(C(F)(F)F)cc2NS(=O)(=O)c2ccc(Cl)cc2)n1 10.1016/j.bmcl.2012.09.020
71454246 83981 None 0 Human Binding pKi = 6.3 6.3 1 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
CHEMBL2207089 83981 None 0 Human Binding pKi = 6.3 6.3 1 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
155522058 170642 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4451290 170642 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
155522058 170642 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4451290 170642 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 379 5 2 5 3.0 Nc1nc2[nH]c(CCc3ccccc3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
781 3394 None 80 Human Binding pKi = 6.3 6.3 - 1
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 6.3 6.3 - 1
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 6.3 6.3 - 1
Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
118734675 118698 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccc(C#N)c4)ccc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417220 118698 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 571 5 1 3 7.6 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3cc(-c4cccc(C#N)c4)ccc32)C1 10.1016/j.ejmech.2015.01.063
89823462 126356 None 0 Human Binding pKi = 6.3 6.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
CHEMBL3650404 126356 None 0 Human Binding pKi = 6.3 6.3 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 463 4 1 6 2.5 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3C(=O)OC(C)(C)C)C1 nan
10436045 3514 None 4 Human Binding pKi = 6.3 6.3 -85 13
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 6.3 6.3 -85 13
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 6.3 6.3 -85 13
Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
22335665 173465 None 0 Human Binding pKi = 7.2 7.2 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 173465 None 0 Human Binding pKi = 7.2 7.2 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
22335665 173465 None 0 Human Binding pKi = 7.2 7.2 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4529804 173465 None 0 Human Binding pKi = 7.2 7.2 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 331 3 1 3 3.8 CC(=O)C1=C(O)C(=O)N(c2ccc(C)c(F)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
781 3394 None 80 Human Binding pKi = 7.2 7.2 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 7.2 7.2 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 7.2 7.2 - 1
Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
3013430 21129 None 1 Human Binding pKi = 6.2 6.2 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 6.2 6.2 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
89823427 126308 None 0 Human Binding pKi = 6.2 6.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
CHEMBL3650358 126308 None 0 Human Binding pKi = 6.2 6.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 509 5 1 7 2.6 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ncn2)C1 nan
162658125 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
10111333 175465 None 0 Human Binding pKi = 8.2 8.2 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4577133 175465 None 0 Human Binding pKi = 8.2 8.2 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 395 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
89823620 126361 None 0 Human Binding pKi = 8.2 8.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650409 126361 None 0 Human Binding pKi = 8.2 8.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 506 5 1 5 4.2 CC[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
162658125 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
162658125 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4760108 181094 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting methodDisplacement of [3H]-CCR2-RA-(R) from human CCR2b expressed in human U2OS cell membranes pre-incubated for 4 hrs before radio ligand addition and measured after 20 mins by scintillation counting method
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1 10.1021/acs.jmedchem.0c01137
155531561 171648 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4466027 171648 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155531561 171648 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4466027 171648 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 359 6 2 5 3.2 CCC(CC)Cc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
183790 3740 None 11 Human Binding pKi = 8.2 8.2 -6 2
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 8.2 8.2 -6 2
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 8.2 8.2 -6 2
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
89823439 126297 None 0 Human Binding pKi = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650347 126297 None 0 Human Binding pKi = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
183790 3740 None 11 Human Binding pKi = 7.2 7.2 -6 2
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.6b01309
783 3740 None 11 Human Binding pKi = 7.2 7.2 -6 2
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.6b01309
CHEMBL1178786 3740 None 11 Human Binding pKi = 7.2 7.2 -6 2
Binding affinity to CCR2 (unknown origin) assessed as inhibition constantBinding affinity to CCR2 (unknown origin) assessed as inhibition constant
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/acs.jmedchem.6b01309
71456008 83987 None 0 Human Binding pKi = 7.2 7.2 25 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207095 83987 None 0 Human Binding pKi = 7.2 7.2 25 3
Binding affinity to CCR2 by 35S-gamma-GTP membrane assayBinding affinity to CCR2 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
162672927 183181 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4795646 183181 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
44309012 102821 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102821 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
44309012 102821 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
CHEMBL305470 102821 None 0 Human Binding pKi = 6.2 6.2 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 9 3 3 6.9 O=C(/C=C/c1ccc(Cl)c(Cl)c1)NCCCCCN1[C@H]2CC[C@@H]1CC(c1c[nH]c3ccc(O)cc13)C2 10.1016/s0960-894x(01)00397-3
781 3394 None 80 Human Binding pKi = 5.2 5.2 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 5.2 5.2 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 5.2 5.2 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9967166 169971 None 11 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 169971 None 11 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
118723408 116321 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 517 7 2 4 4.8 COc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
CHEMBL3359297 116321 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 517 7 2 4 4.8 COc1cccc(C2CCC(N3CCC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)CC3)CC2)c1 10.1016/j.bmcl.2014.10.060
9967166 169971 None 11 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
CHEMBL4441958 169971 None 11 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 4 1 3 3.9 CCc1ccc(N2C(=O)C(O)=C(C(C)=O)C2C2CCCCC2)cc1 10.1021/acs.jmedchem.8b00605
155559153 174779 None 0 Human Binding pKi = 7.2 7.2 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174779 None 0 Human Binding pKi = 7.2 7.2 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
89823506 126334 None 0 Human Binding pKi = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
CHEMBL3650384 126334 None 0 Human Binding pKi = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 532 5 1 6 3.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(C#N)c(C(F)(F)F)c2)C1 nan
155559153 174779 None 0 Human Binding pKi = 7.2 7.2 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
CHEMBL4561618 174779 None 0 Human Binding pKi = 7.2 7.2 -2 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 457 4 1 3 5.6 O=C(C1=C(O)C(=O)N(c2ccc(Br)cc2F)C1C1CCCCC1)c1ccccc1 10.1021/acs.jmedchem.8b00605
44353447 3773 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
89823342 126357 None 0 Human Binding pKi = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
CHEMBL3650405 126357 None 0 Human Binding pKi = 7.2 7.2 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 492 4 1 5 3.9 C[C@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccn2)C1 nan
3013430 21129 None 1 Human Binding pKi = 7.2 7.2 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 7.2 7.2 - 1
Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
155553573 174175 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4547381 174175 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
155553573 174175 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4547381 174175 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric methodDisplacement of [3H]-CCR2-RA-[R] from human CCR2 expressed in human U2OS cells incubated for 2 hrs by scintillation spectrometric method
ChEMBL 345 6 2 5 3.0 CCCCCc1[nH]c2nc(N)nn2c(=O)c1Cc1cccc(Cl)c1 10.1021/acs.jmedchem.9b00742
118734583 118693 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(Cl)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL3417123 118693 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 504 4 1 2 6.7 CC(C)[C@]1(C(=O)N2CCc3ccc(C(F)(F)F)cc3C2)CC[C@@H](NC2CCc3ccc(Cl)cc32)C1 10.1016/j.ejmech.2015.01.063
CHEMBL11359 9778 None 0 Human Binding pKi = 5.2 5.2 -2 4
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL None None None None nan
44353447 3773 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
10436045 3514 None 4 Human Binding pKi = 6.1 6.1 -85 13
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
782 3514 None 4 Human Binding pKi = 6.1 6.1 -85 13
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
CHEMBL432713 3514 None 4 Human Binding pKi = 6.1 6.1 -85 13
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1021/jm030862l
118723021 116265 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 487 6 2 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3358698 116265 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 487 6 2 3 4.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccccc3)CC2)CC1 10.1016/j.bmcl.2014.10.060
118734679 118701 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1ccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)cc1 10.1016/j.ejmech.2015.01.063
CHEMBL3417224 118701 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 576 6 1 3 7.7 COc1ccc(-c2ccc3c(c2)CCC3N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)cc1 10.1016/j.ejmech.2015.01.063
3013430 21129 None 1 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
CHEMBL131243 21129 None 1 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 480 6 1 3 6.6 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CCC3)cc1 10.1021/jm030862l
89823417 126343 None 0 Human Binding pKi = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
CHEMBL3650392 126343 None 0 Human Binding pKi = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 498 5 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccc(Cl)c(C#N)c2)C1 nan
44353447 3773 None 0 Human Binding pKi = 5.1 5.1 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
785 3773 None 0 Human Binding pKi = 5.1 5.1 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
CHEMBL337246 3773 None 0 Human Binding pKi = 5.1 5.1 - 1
Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/jm030862l
89823348 126346 None 0 Human Binding pKi = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
CHEMBL3650395 126346 None 0 Human Binding pKi = 7.1 7.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 575 5 1 5 4.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2cc(C(F)(F)F)ccc2C(F)(F)F)C1 nan
25110660 154870 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154870 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
9857981 170785 None 11 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170785 None 11 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
25110660 154870 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL400698 154870 None 0 Human Binding pKi = 7.1 7.1 - 1
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cellsInhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
ChEMBL 525 6 3 3 6.7 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2CCC(c3c[nH]c4ccc(O)cc34)CC2)CC1 10.1016/s0960-894x(01)00397-3
89823541 126321 None 0 Human Binding pKi = 6.1 6.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
CHEMBL3650371 126321 None 0 Human Binding pKi = 6.1 6.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 508 5 1 6 3.2 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2ccnc(C(F)(F)F)c2)C1 nan
89823450 126344 None 0 Human Binding pKi = 8.1 8.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
CHEMBL3650393 126344 None 0 Human Binding pKi = 8.1 8.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 562 4 0 4 6.2 N#Cc1ccc(C(F)(F)F)cc1N1C[C@@H]2C[C@H]1CN2C(=O)[C@@]12CCC[C@@H]1C[C@@H](N1CCC(c3ccccc3)CC1)C2 nan
22725647 173697 None 0 Human Binding pKi = 8.1 8.1 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173697 None 0 Human Binding pKi = 8.1 8.1 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
9857981 170785 None 11 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4453024 170785 None 11 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 313 3 1 3 3.7 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
118734689 118711 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 606 6 1 3 7.8 CCC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2cc(OC)c(Br)cc21 10.1016/j.ejmech.2015.01.063
CHEMBL3417234 118711 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometryDisplacement of 0.1 nM [125I]CCL2 from human CCR2 expressing human U2OS cell membrane by scintillation spectrometry
ChEMBL 606 6 1 3 7.8 CCC1CC(N[C@@H]2CC[C@@](C(=O)N3CCc4ccc(C(F)(F)F)cc4C3)(C(C)C)C2)c2cc(OC)c(Br)cc21 10.1016/j.ejmech.2015.01.063
89823428 126325 None 0 Human Binding pKi = 6.1 6.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
CHEMBL3650375 126325 None 0 Human Binding pKi = 6.1 6.1 - 1
Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).Radioligand Binding Assay: Radioligand binding assays were performed in CHO cells expressing human CCR2B and Galpha±16 coupling protein. All compounds were dissolved in DMSO and assays run at a final DMSO concentration of 0.5% (v/v). [125I]-labeled human MCP-1 was purchased from PerkinElmer. Unlabelled human MCP-1 was purchased from PeproTech.Compounds were serially diluted in DMSO before diluting into assay buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) with cryo preserved CHO cells expressing human CCR2B and the Galpha±16 coupling protein (30x103/well) and [125I]-MCP-1 (50 pM). The reaction was incubated at room temperature for 90 minutes before transferring to GF/C filter membrane (PerkinElmer) pre-treated with 0.3% polyethyleneimine for 2 hours at 4 C. The filter membrane was washed six times with ice cold wash buffer (25 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 500 mM NaCl, 0.01% (m/v) azide), dried, and sealed in a RLB sample bag (Agilent Technologies).
ChEMBL 514 5 1 7 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1C[C@H]2CCC[C@@]2(C(=O)N2C[C@@H]3C[C@H]2CN3c2nc(C(F)(F)F)cs2)C1 nan
4485 69377 None 118 Human Binding pKi = 6.1 6.1 -1 8
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
CHEMBL193 69377 None 118 Human Binding pKi = 6.1 6.1 -1 8
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] nan
781 3394 None 80 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
9953769 3394 None 80 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
CHEMBL134074 3394 None 80 Human Binding pKi = 6.1 6.1 - 1
Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 10.1021/jm030862l
162672927 183181 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
CHEMBL4795646 183181 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-CCR2-RA from human CCR2b expressed in human U2OS cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 733 11 3 7 6.4 O=C(NCCNC(=O)c1ccc(S(=O)(=O)F)cc1)c1ccc(Oc2ccc(Cl)cc2NS(=O)(=O)c2ccc(Cl)c(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.0c01137
22725647 173697 None 0 Human Binding pKi = 8.1 8.1 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4535696 173697 None 0 Human Binding pKi = 8.1 8.1 3 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 347 3 1 3 4.3 CC(=O)C1=C(O)C(=O)N(c2ccc(Cl)c(C)c2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
183790 3740 None 11 Human Binding pKi = 8.0 8.0 -6 2
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
783 3740 None 11 Human Binding pKi = 8.0 8.0 -6 2
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
CHEMBL1178786 3740 None 11 Human Binding pKi = 8.0 8.0 -6 2
Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cellsBinding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1021/jm030862l
118723412 116323 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 531 6 2 5 4.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc4c(c3)OCO4)CC2)CC1 10.1016/j.bmcl.2014.10.060
CHEMBL3359301 116323 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assayDisplacement of [125I]CCL2 from CCR2 in human U2OS cell membranes by radioligand displacement assay
ChEMBL 531 6 2 5 4.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCN(C2CCC(c3ccc4c(c3)OCO4)CC2)CC1 10.1016/j.bmcl.2014.10.060
10133557 172537 None 0 Human Binding pKi = 7.0 7.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 172537 None 0 Human Binding pKi = 7.0 7.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
10133557 172537 None 0 Human Binding pKi = 7.0 7.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4483771 172537 None 0 Human Binding pKi = 7.0 7.0 1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 367 3 1 3 4.4 CC(=O)C1=C(O)C(=O)N(c2ccc(C(F)(F)F)cc2)C1C1CCCCC1 10.1021/acs.jmedchem.8b00605
8447 188947 None 84 Human Binding pKi = 6.0 6.0 -12 13
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188947 None 84 Human Binding pKi = 6.0 6.0 -12 13
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
9945265 171181 None 0 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 171181 None 0 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
3117 207839 None 103 Human Binding pKi = 6.0 6.0 -2 16
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207839 None 103 Human Binding pKi = 6.0 6.0 -2 16
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
9945265 171181 None 0 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
CHEMBL4459033 171181 None 0 Human Binding pKi = 7.0 7.0 -1 2
Displacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometryDisplacement of [3H]-CCR2-RA-[R] from human TEV protease site linked CCR2b expressed in human U20S cell membranes co-expressing Gal4-VP16 transcription factor after 120 mins by scintillation spectrometry
ChEMBL 327 3 1 3 4.1 CC(=O)C1=C(O)C(=O)N(c2ccc(C)cc2)C1C1CCCCCC1 10.1021/acs.jmedchem.8b00605
46208367 83579 None 13 Mouse Binding pKi = 5.0 5.0 - 1
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
CHEMBL2204263 83579 None 13 Mouse Binding pKi = 5.0 5.0 - 1
Binding affinity to mouse CCR2Binding affinity to mouse CCR2
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3cncs3)CC2)C1 10.1021/ml300260s
12093170 871 None 31 Human Binding pIC50 < 5.3 5.3 - 1
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
9431 871 None 31 Human Binding pIC50 < 5.3 5.3 - 1
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
CHEMBL4519152 871 None 31 Human Binding pIC50 < 5.3 5.3 - 1
Antagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cellsAntagonism of <sup>125</sup>I-MCP-1 binding to THP-1 cells
Guide to Pharmacology 351 3 1 3 4.2 Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C None
4410 3135 None 106 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015 3135 None 106 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
844 3135 None 106 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
CHEMBL18442 3135 None 106 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
DB06809 3135 None 106 Human Binding pIC50 = 8.0 8.0 - 1
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cellsDisplacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
11598 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
23725177 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
CHEMBL4442783 672 None 9 Human Binding pIC50 = 9.0 9.0 - 1
Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.
Guide to Pharmacology 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 30891130
10586 2137 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
11617815 2137 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
CHEMBL5290248 2137 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.Measuring antagonism of <sup>125</sup>I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.
Guide to Pharmacology 379 5 1 6 4.3 CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F 18599682
46198579 3060 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
9979 3060 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
DB14955 3060 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.
Guide to Pharmacology 511 6 1 7 2.9 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F None
176 398 None 66 Human Binding pKi = 8.3 8.3 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 398 None 66 Human Binding pKi = 8.3 8.3 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 398 None 66 Human Binding pKi = 8.3 8.3 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 398 None 66 Human Binding pKi = 8.3 8.3 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 398 None 66 Human Binding pKi = 8.3 8.3 -3 31
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
3117 207839 None 103 Human Binding pKi = 8.2 8.2 -2 16
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 207839 None 103 Human Binding pKi = 8.2 8.2 -2 16
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
4485 69377 None 118 Human Binding pKi = 8.2 8.2 -1 8
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] None
CHEMBL193 69377 None 118 Human Binding pKi = 8.2 8.2 -1 8
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
Drug Central 346 4 1 7 2.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1c1ccccc1[N+](=O)[O-] None
10585 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
145996522 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
CHEMBL4531005 1078 None 1 Human Binding pKi = 8.8 8.8 - 1
Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.Binding affinity determined from a radioligand binding assay, measuring displacement of [<sup>3</sup>H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.
Guide to Pharmacology 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 31742400
11560568 1884 None 0 Human Binding pKi = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
3502 1884 None 0 Human Binding pKi = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
CHEMBL1082152 1884 None 0 Human Binding pKi = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 409 6 4 6 1.7 OCC(CNc1cccc(c1)C1=C(C(=O)NC1=O)c1cn(c2c1cc(F)cc2)C)O None
44353447 3773 None 0 Human Binding pKi None 6.5 6.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
785 3773 None 0 Human Binding pKi None 6.5 6.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
CHEMBL337246 3773 None 0 Human Binding pKi None 6.5 6.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 12954060
781 3394 None 80 Human Binding pKi None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
9953769 3394 None 80 Human Binding pKi None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
CHEMBL134074 3394 None 80 Human Binding pKi None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 417 4 1 5 5.1 O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C 12954060
10436045 3514 None 4 Human Binding pKi None 7 7.0 -85 13
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
782 3514 None 4 Human Binding pKi None 7 7.0 -85 13
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
CHEMBL432713 3514 None 4 Human Binding pKi None 7 7.0 -85 13
UnclassifiedUnclassified
Guide to Pharmacology 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 12954060
183790 3740 None 11 Human Binding pKi None 7.2 7.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
783 3740 None 11 Human Binding pKi None 7.2 7.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
CHEMBL1178786 3740 None 11 Human Binding pKi None 7.2 7.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
183790 3740 None 11 Human Binding pKi None 8.2 8.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
183790 3740 None 11 Human Binding pKi None 8.2 8.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
783 3740 None 11 Human Binding pKi None 8.2 8.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
783 3740 None 11 Human Binding pKi None 8.2 8.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060
CHEMBL1178786 3740 None 11 Human Binding pKi None 8.2 8.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10318947
CHEMBL1178786 3740 None 11 Human Binding pKi None 8.2 8.2 -6 2
UnclassifiedUnclassified
Guide to Pharmacology 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 12954060