Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
44252324 149166 1 None 42 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None 42 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None 42 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None 42 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None 42 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None 42 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None 42 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None 42 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None 151 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None 151 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None 42 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None 42 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
58509355 149421 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 507 7 2 5 3.4 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3891692 149421 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 507 7 2 5 3.4 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2016.09.047
58509356 159354 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 439 7 2 5 2.6 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCCCC1 10.1016/j.bmcl.2016.09.047
CHEMBL3971826 159354 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 439 7 2 5 2.6 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCCCC1 10.1016/j.bmcl.2016.09.047
58509165 154653 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 457 7 2 6 2.6 Cc1ccc(S(=O)(=O)NC(CCn2cccc2C#N)C(=O)N2CCC(C)CC2)c(C)c1N 10.1016/j.bmcl.2016.09.047
CHEMBL3933303 154653 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 457 7 2 6 2.6 Cc1ccc(S(=O)(=O)NC(CCn2cccc2C#N)C(=O)N2CCC(C)CC2)c(C)c1N 10.1016/j.bmcl.2016.09.047
44252464 153445 0 None -89 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3923733 153445 0 None -89 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2016.09.047
58504873 153738 0 None -17 2 Mouse 5.0 pIC50 = 5 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 483 7 2 4 4.1 CC1CCN(C(=O)[C@@H](CCc2ccccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3926111 153738 0 None -17 2 Mouse 5.0 pIC50 = 5 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 483 7 2 4 4.1 CC1CCN(C(=O)[C@@H](CCc2ccccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None 151 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None 151 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None 151 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None 151 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58504900 149368 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 517 7 2 4 4.8 CC1CCN(C(=O)C(CCc2ccccc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3891289 149368 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 517 7 2 4 4.8 CC1CCN(C(=O)C(CCc2ccccc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58508974 156195 0 None 50 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 467 7 1 6 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3c2ccn3C)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3945769 156195 0 None 50 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 467 7 1 6 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3c2ccn3C)CC1 10.1016/j.bmcl.2016.09.047
58509106 158083 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 455 7 3 6 1.6 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCC(O)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3960700 158083 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 455 7 3 6 1.6 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCC(O)CC1 10.1016/j.bmcl.2016.09.047
58509273 150047 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 414 7 1 5 2.4 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3896799 150047 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 414 7 1 5 2.4 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.09.047
58509102 159061 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 483 7 2 6 3.0 N#Cc1cccn1CCC(NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1)C(=O)N1CCCCC1 10.1016/j.bmcl.2016.09.047
CHEMBL3969321 159061 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 483 7 2 6 3.0 N#Cc1cccn1CCC(NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1)C(=O)N1CCCCC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None 151 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP productionAntagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP production
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None 151 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP productionAntagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP production
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509238 156608 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 473 7 2 6 2.8 CC1CCN(C(=O)C(CCn2cccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3948828 156608 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 473 7 2 6 2.8 CC1CCN(C(=O)C(CCn2cccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None -151 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None -151 2 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
134155728 157810 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)[C@H](CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3958582 157810 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)[C@H](CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None -42 2 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None -42 2 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
58509160 152800 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 3.0 CC1CCCCN1C(=O)C(CCn1cccc1C#N)NS(=O)(=O)c1cccc2[nH]ccc12 10.1016/j.bmcl.2016.09.047
CHEMBL3918664 152800 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 3.0 CC1CCCCN1C(=O)C(CCn1cccc1C#N)NS(=O)(=O)c1cccc2[nH]ccc12 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
44252468 159368 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3971886 159368 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2016.09.047
58509377 151628 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 3.0 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCCCCC1 10.1016/j.bmcl.2016.09.047
CHEMBL3909737 151628 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 3.0 N#Cc1cccn1CCC(NS(=O)(=O)c1cccc2[nH]ccc12)C(=O)N1CCCCCC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None 42 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP productionAntagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP production
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None 42 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP productionAntagonist activity at human CCR10 expressed in HEK cells assessed as inhibition of human CCL27-dependent cAMP production
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None -42 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None -42 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
58509350 151436 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908230 151436 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by FLIPR assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509048 150560 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.4 N#Cc1cccn1CCC(NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1)C(=O)N1CCCCCC1 10.1016/j.bmcl.2016.09.047
CHEMBL3901006 150560 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.4 N#Cc1cccn1CCC(NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1)C(=O)N1CCCCCC1 10.1016/j.bmcl.2016.09.047
66883409 155768 0 None 31 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3cc[nH]c23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3942284 155768 0 None 31 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3cc[nH]c23)CC1 10.1016/j.bmcl.2016.09.047
58509301 160309 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 507 7 2 6 3.4 CC1CCN(C(=O)C(CCn2nccc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3979967 160309 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 507 7 2 6 3.4 CC1CCN(C(=O)C(CCn2nccc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
145957924 168872 0 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 886 20 2 10 3.4 CC[C@H](C)[C@@H](OC(=O)/C=C\c1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
CHEMBL4161021 168872 0 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 886 20 2 10 3.4 CC[C@H](C)[C@@H](OC(=O)/C=C\c1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
145952624 169164 0 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 889 21 2 10 3.3 CC[C@H](C)[C@@H](OC(=O)CCc1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
CHEMBL4165525 169164 0 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 889 21 2 10 3.3 CC[C@H](C)[C@@H](OC(=O)CCc1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
44252324 149166 1 None 42 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None 42 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
58509125 155984 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 474 7 2 7 2.2 CC1CCN(C(=O)C(CCn2nccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3943972 155984 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 474 7 2 7 2.2 CC1CCN(C(=O)C(CCn2nccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509038 152879 0 None -50 2 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 498 7 2 7 2.6 CC1CCN(C(=O)C(CCn2nccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3919363 152879 0 None -50 2 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 498 7 2 7 2.6 CC1CCN(C(=O)C(CCn2nccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509203 157959 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2c(N)cc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3959737 157959 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2c(N)cc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2016.09.047
58509058 156343 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 551 7 2 6 3.8 N#Cc1cccn1CCC(NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1)C(=O)N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3946799 156343 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 551 7 2 6 3.8 N#Cc1cccn1CCC(NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1)C(=O)N1CCC(C(F)(F)F)CC1 10.1016/j.bmcl.2016.09.047
58508981 155566 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 472 7 2 5 3.4 CC1CCN(C(=O)C(CCn2cccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3940706 155566 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 472 7 2 5 3.4 CC1CCN(C(=O)C(CCn2cccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
134152132 160299 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 399 7 2 5 1.7 CN(C)C(=O)C(CCn1cccc1C#N)NS(=O)(=O)c1cccc2[nH]ccc12 10.1016/j.bmcl.2016.09.047
CHEMBL3979899 160299 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 399 7 2 5 1.7 CN(C)C(=O)C(CCn1cccc1C#N)NS(=O)(=O)c1cccc2[nH]ccc12 10.1016/j.bmcl.2016.09.047
145953024 169369 0 None 4 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 886 20 2 10 3.4 CC[C@H](C)[C@@H](OC(=O)/C=C/c1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
CHEMBL4168948 169369 0 None 4 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence methodAntagonist activity at human CCR10 expressed in human U2OS cells assessed as inhibition of CCL27-induced beta-arrestin recruitment pre-incubated for 30 mins before CCL27 stimulation for 90 or 180 mins by chemiluminescence method
ChEMBL 886 20 2 10 3.4 CC[C@H](C)[C@@H](OC(=O)/C=C/c1ccccc1)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)OC 10.1021/acs.jmedchem.8b00885
58509360 159739 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 464 7 1 5 3.5 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3975141 159739 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 464 7 1 5 3.5 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2016.09.047
134132126 151528 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)[C@@H](CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908983 151528 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)[C@@H](CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509026 156943 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 498 7 2 7 2.6 CC1CCN(C(=O)C(CCn2ccnc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951650 156943 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 498 7 2 7 2.6 CC1CCN(C(=O)C(CCn2ccnc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509147 158512 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 507 7 2 6 3.4 CC1CCN(C(=O)C(CCn2ccnc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3964547 158512 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 507 7 2 6 3.4 CC1CCN(C(=O)C(CCn2ccnc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509216 149287 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)C1 10.1016/j.bmcl.2016.09.047
CHEMBL3890608 149287 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)C1 10.1016/j.bmcl.2016.09.047
58509038 152879 0 None 50 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 498 7 2 7 2.6 CC1CCN(C(=O)C(CCn2nccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3919363 152879 0 None 50 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 498 7 2 7 2.6 CC1CCN(C(=O)C(CCn2nccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509138 158088 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)cc2Cl)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3960764 158088 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)cc2Cl)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None -42 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None -42 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
58509350 151436 2 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908230 151436 2 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58504873 153738 0 None 17 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 483 7 2 4 4.1 CC1CCN(C(=O)[C@@H](CCc2ccccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3926111 153738 0 None 17 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 483 7 2 4 4.1 CC1CCN(C(=O)[C@@H](CCc2ccccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509063 157423 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)C1 10.1016/j.bmcl.2016.09.047
CHEMBL3955499 157423 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)C1 10.1016/j.bmcl.2016.09.047
58508974 156195 0 None -50 2 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 467 7 1 6 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3c2ccn3C)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3945769 156195 0 None -50 2 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 467 7 1 6 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3c2ccn3C)CC1 10.1016/j.bmcl.2016.09.047
58509350 151436 2 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908230 151436 2 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
134135125 150960 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)[C@@H](CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3904154 150960 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)[C@@H](CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
44252464 153445 0 None 89 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3923733 153445 0 None 89 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2016.09.047
58509246 153948 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.4 CC1CCCCN1C(=O)C(CCn1cccc1C#N)NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1 10.1016/j.bmcl.2016.09.047
CHEMBL3927890 153948 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 497 7 2 6 3.4 CC1CCCCN1C(=O)C(CCn1cccc1C#N)NS(=O)(=O)c1cc(Cl)c(N)c(Cl)c1 10.1016/j.bmcl.2016.09.047
58509350 151436 2 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908230 151436 2 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by FLIPR assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509350 151436 2 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908230 151436 2 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assayAntagonist activity at human CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of human CCL28-dependent calcium flux by chemiluminescence assay
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
66883409 155768 0 None -31 2 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3cc[nH]c23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3942284 155768 0 None -31 2 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assayAntagonist activity at mouse CCR10 expressed in CHOK1 cells coexpressing aequorin/Galphaq assessed as inhibition of CCL27-dependent calcium flux in presence of coelenterazine H by chemiluminescence assay
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3cc[nH]c23)CC1 10.1016/j.bmcl.2016.09.047
131801164 7416 0 None -25 2 Mouse 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 453 7 2 5 2.8 N#Cc1cccn1CC[C@H](C(=O)N1CCC(CC1)C)NS(=O)(=O)c1cccc2c1cc[nH]2 27692854
9714 7416 0 None -25 2 Mouse 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 453 7 2 5 2.8 N#Cc1cccn1CC[C@H](C(=O)N1CCC(CC1)C)NS(=O)(=O)c1cccc2c1cc[nH]2 27692854
131801164 7416 0 None 25 2 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 453 7 2 5 2.8 N#Cc1cccn1CC[C@H](C(=O)N1CCC(CC1)C)NS(=O)(=O)c1cccc2c1cc[nH]2 27692854
9714 7416 0 None 25 2 Human 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 453 7 2 5 2.8 N#Cc1cccn1CC[C@H](C(=O)N1CCC(CC1)C)NS(=O)(=O)c1cccc2c1cc[nH]2 27692854




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
44252324 149166 1 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
44252324 149166 1 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP bindingAntagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP binding
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3889627 149166 1 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP bindingAntagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP binding
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2016.09.047
44252468 159368 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3971886 159368 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2016.09.047
58509125 155984 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 474 7 2 7 2.2 CC1CCN(C(=O)C(CCn2nccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3943972 155984 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 474 7 2 7 2.2 CC1CCN(C(=O)C(CCn2nccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509238 156608 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 473 7 2 6 2.8 CC1CCN(C(=O)C(CCn2cccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3948828 156608 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 473 7 2 6 2.8 CC1CCN(C(=O)C(CCn2cccn2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
44252464 153445 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3923733 153445 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 453 7 2 5 2.8 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP bindingAntagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP binding
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP bindingAntagonist activity at human CCR10 expressed in HEK cell membranes assessed as inhibition of human CCL27-dependent europium-labeled GTP binding
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509147 158512 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 507 7 2 6 3.4 CC1CCN(C(=O)C(CCn2ccnc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3964547 158512 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 507 7 2 6 3.4 CC1CCN(C(=O)C(CCn2ccnc2Cl)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysisDisplacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysis
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysisDisplacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysis
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysisDisplacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysis
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysisDisplacement of human CCL27-Fc from CCR10 expressed in HEK cell membranes by immunochemical binding analysis
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509213 156883 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Reversible inhibition of human CCL27-Fc binding to CCR10 expressed in HEK cell membranes by immunochemical binding assayReversible inhibition of human CCL27-Fc binding to CCR10 expressed in HEK cell membranes by immunochemical binding assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3951018 156883 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Reversible inhibition of human CCL27-Fc binding to CCR10 expressed in HEK cell membranes by immunochemical binding assayReversible inhibition of human CCL27-Fc binding to CCR10 expressed in HEK cell membranes by immunochemical binding assay
ChEMBL 497 7 2 6 3.2 CC1CCN(C(=O)C(CCn2cccc2C#N)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509350 151436 2 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908230 151436 2 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58504873 153738 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 483 7 2 4 4.1 CC1CCN(C(=O)[C@@H](CCc2ccccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3926111 153738 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 483 7 2 4 4.1 CC1CCN(C(=O)[C@@H](CCc2ccccc2)NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509350 151436 2 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
CHEMBL3908230 151436 2 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 518 8 2 8 2.7 CC1CCN(C(=O)C(CCn2ccnc2[N+](=O)[O-])NS(=O)(=O)c2cc(Cl)c(N)c(Cl)c2)CC1 10.1016/j.bmcl.2016.09.047
58509165 154653 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 457 7 2 6 2.6 Cc1ccc(S(=O)(=O)NC(CCn2cccc2C#N)C(=O)N2CCC(C)CC2)c(C)c1N 10.1016/j.bmcl.2016.09.047
CHEMBL3933303 154653 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxisAntagonist activity at human CCR10 expressed in mouse BA/F3 cells assessed as inhibition of human CCL27-dependent chemotaxis
ChEMBL 457 7 2 6 2.6 Cc1ccc(S(=O)(=O)NC(CCn2cccc2C#N)C(=O)N2CCC(C)CC2)c(C)c1N 10.1016/j.bmcl.2016.09.047