Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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
CHEMBL2064011 215950 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL1170042 215327 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170045 215330 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170640 215350 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170231 215337 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL5081621 221535 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170045 215330 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170231 215337 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170635 215345 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170635 215345 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
101886248 121752 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 121752 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
44426497 92510 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229006 92510 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170026 215318 0 None 48 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
3915 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
49799079 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5760 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
91933514 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170027 215319 0 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
44426495 92509 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229005 92509 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL5080181 221447 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
101886248 121752 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 121752 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL1170026 215318 0 None 48 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
3915 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
49799079 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5760 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
91933514 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170027 215319 0 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL5075364 221149 0 None -2511 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL2064020 215959 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
122392665 172220 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ releaseAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release
ChEMBL 457 10 6 5 3.3 N=C(N)NCCC[C@H](Nc1nccc2[nH]c(C(c3ccccc3)c3ccccc3)nc12)C(=O)O 10.1021/acs.jmedchem.7b00882
CHEMBL4239035 172220 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ releaseAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release
ChEMBL 457 10 6 5 3.3 N=C(N)NCCC[C@H](Nc1nccc2[nH]c(C(c3ccccc3)c3ccccc3)nc12)C(=O)O 10.1021/acs.jmedchem.7b00882
17753143 92715 4 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL230034 92715 4 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430551 94779 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234305 94779 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL1170025 215317 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
44426475 151447 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL390834 151447 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL2064012 215951 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
71525749 143207 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 143207 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71525749 143207 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 143207 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5080381 221460 0 None -47 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170025 215317 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170043 215328 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71768012 143230 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 143230 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71768012 143230 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 143230 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44426496 148820 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL387755 148820 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL2063898 215949 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
44430554 158048 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396031 158048 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430547 175638 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL438129 175638 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL1170029 215321 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
11252 7557 39 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 7557 39 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 7557 39 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL1170034 215325 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O 10.1021/jm1003705
CHEMBL1170043 215328 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
8381 7816 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
91827354 7816 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL3342689 7816 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL1170029 215321 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170034 215325 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O 10.1021/jm1003705
CHEMBL2064018 215957 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
89570392 143255 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 143255 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570392 143255 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 143255 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1169838 215316 0 None -6 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170433 215341 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
8381 7816 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
91827354 7816 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL3342689 7816 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL2064016 215955 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL1170433 215341 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170229 215335 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1169838 215316 0 None -6 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170229 215335 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
71566581 143282 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 143282 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170643 215352 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL2064018 215957 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Partial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerPartial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
71566581 143282 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 143282 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170643 215352 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL5092449 222147 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170648 215355 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170648 215355 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5087237 221859 0 None -446 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.1c01174
CHEMBL1170437 215343 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170437 215343 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170638 215348 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170035 215326 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170638 215348 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at C3aR in human MDM cells assessed as Ca2+ responseAgonist activity at C3aR in human MDM cells assessed as Ca2+ response
ChEMBL None None None None 10.1016/j.bmcl.2015.10.038
CHEMBL1170638 215348 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170035 215326 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL2064014 215953 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL2064019 215958 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL1170641 215351 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170641 215351 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170650 215356 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/jm1003705
CHEMBL5080234 221450 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170637 215347 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170650 215356 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170637 215347 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5085743 221765 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170030 215322 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170221 215333 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170223 215334 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
101886250 121753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 121753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
49799093 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5761 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1172879 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170030 215322 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170221 215333 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
44426472 92479 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228847 92479 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170223 215334 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
101886250 121753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 121753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
127036518 143153 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 143153 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127036518 143153 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 143153 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
49799093 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5761 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1172879 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5082686 221599 0 None -275 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC[C@@H](C)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL5093227 222196 0 None -99 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
127034744 143184 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735339 143184 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL1170438 215344 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170438 215344 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 215342 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 215342 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL2064017 215956 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerAgonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL1170636 215346 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170636 215346 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
71565510 143171 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 143171 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566652 143316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 143316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44426463 93169 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL231405 93169 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
71565510 143171 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 143171 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566652 143316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 143316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170044 215329 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1173027 215368 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170639 215349 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170232 215338 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170639 215349 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
117634952 143312 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 143312 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170232 215338 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
117634952 143312 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 143312 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170044 215329 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5083558 221649 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)N)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
71565582 143232 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 143232 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565582 143232 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 143232 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1173027 215368 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5078171 221318 0 None -436 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL5071478 221038 6 None -933 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
71566653 143208 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 143208 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566653 143208 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 143208 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170028 215320 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL2021602 215909 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm1003705
CHEMBL2021602 215909 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm1003705
CHEMBL1170046 215331 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5085196 221734 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170046 215331 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5081287 221518 0 None 30 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)N)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL2064017 215956 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL2064019 215958 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerPartial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL2064013 215952 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL1170349 215339 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170349 215339 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5092461 222149 0 None -2041 2 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.1c01174
71566654 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assayAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1021/acs.jmedchem.7b00882
9449 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assayAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1021/acs.jmedchem.7b00882
CHEMBL3736108 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assayAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1021/acs.jmedchem.7b00882
71566654 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
71566654 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 7792 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
71565580 143262 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 143262 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5079833 221425 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL2064015 215954 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
71565506 143254 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 143254 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170220 215332 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565506 143254 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 143254 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634979 143133 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 143133 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634979 143133 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 143133 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5092578 222155 0 None -295 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1169603 215315 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL2064016 215955 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerAgonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
44430549 158045 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396030 158045 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL1169603 215315 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170220 215332 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565580 143262 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 143262 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL2064021 215960 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None None 10.1021/jm201609k
117637102 143308 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 143308 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117637102 143308 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 143308 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5076900 221247 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170230 215336 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170230 215336 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170042 215327 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
8384 7897 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 7897 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 7897 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL2064013 215952 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
10595 8934 21 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
145996525 8934 21 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL4459627 8934 21 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL2064012 215951 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
155525092 177719 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4455385 177719 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155535693 178848 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 486 10 5 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(F)cc2)c2ccc(F)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4472149 178848 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 486 10 5 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(F)cc2)c2ccc(F)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155558856 181594 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 478 12 5 4 3.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(Cc2ccccc2)Cc2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4562412 181594 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 478 12 5 4 3.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(Cc2ccccc2)Cc2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
101886254 121744 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 121744 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
101886249 121745 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 121745 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL2064019 215958 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate readerAntagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL2064021 215960 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None None 10.1021/jm201609k
101886249 121745 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 121745 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
155535683 178850 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472196 178850 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
155554899 181119 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551058 181119 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
3529 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
5311120 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL389348 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
101886254 121744 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 121744 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
127035774 143215 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ responseAntagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ response
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 143215 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ responseAntagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ response
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
3529 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
3529 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
5311120 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL389348 10290 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
155535683 178850 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472196 178850 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
155554899 181119 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551058 181119 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064018 215957 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
17753143 92715 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 92715 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
117634981 121746 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 121746 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
155526496 177913 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4458380 177913 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
17753143 92715 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 92715 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
101886252 121747 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 121747 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
155516924 176929 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
CHEMBL4444281 176929 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
117634981 121746 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 121746 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
155526496 177913 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4458380 177913 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
101886252 121747 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 121747 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
155516924 176929 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
CHEMBL4444281 176929 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
CHEMBL2064011 215950 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155546129 180294 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4530755 180294 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL1170644 215353 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
155555271 181123 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551118 181123 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
155546129 180294 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4530755 180294 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
155555271 181123 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551118 181123 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064019 215958 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
3529 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilizationAntagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
5311120 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilizationAntagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
CHEMBL389348 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilizationAntagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
101886251 121743 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342679 121743 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
155518058 177021 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4445758 177021 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155518058 177021 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4445758 177021 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155510486 181492 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559976 181492 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155557328 181421 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4558167 181421 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155536326 178930 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4473192 178930 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155557328 181421 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4558167 181421 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
44430514 157021 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL395233 157021 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
122392666 172616 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ releaseAntagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ release
ChEMBL 463 9 4 5 3.0 N=C(N)NCCC[C@@H](C(=O)O)N1Cc2nc(C(c3ccccc3)c3ccccc3)sc2C1=O 10.1021/acs.jmedchem.7b00882
CHEMBL4248716 172616 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ releaseAntagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ release
ChEMBL 463 9 4 5 3.0 N=C(N)NCCC[C@@H](C(=O)O)N1Cc2nc(C(c3ccccc3)c3ccccc3)sc2C1=O 10.1021/acs.jmedchem.7b00882
155536326 178930 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4473192 178930 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155557799 181474 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559463 181474 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
101886253 121742 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 121742 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
101886251 121743 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342679 121743 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
3529 10290 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 10290 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 10290 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
155563876 182050 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4572633 182050 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
101886253 121742 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 121742 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
155510486 181492 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559976 181492 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064017 215956 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155557799 181474 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559463 181474 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155563876 182050 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4572633 182050 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL2064014 215953 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL2063898 215949 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155569071 182938 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4592883 182938 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
155569071 182938 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4592883 182938 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
118716617 121741 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 121741 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
155527368 178019 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4459830 178019 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155527368 178019 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4459830 178019 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155534696 178758 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 178758 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
89570464 176598 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4439578 176598 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155535658 178877 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472490 178877 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
CHEMBL2064020 215959 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
89570464 176598 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4439578 176598 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
44430510 165897 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
CHEMBL409773 165897 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
CHEMBL1170028 215320 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
118716617 121741 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 121741 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
155535658 178877 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472490 178877 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
155534696 178758 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 178758 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064015 215954 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
25156014 182228 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 182228 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155534229 178717 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470384 178717 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
8384 7897 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 7897 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 7897 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
155534229 178717 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470384 178717 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
25156014 182228 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 182228 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064018 215957 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate readerAntagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL2064016 215955 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155525092 177719 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4455385 177719 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
127035774 143215 0 None - 1 Human 6.9 pKd = 6.9 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 143215 0 None - 1 Human 6.9 pKd = 6.9 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
127035774 143215 0 None - 1 Human 6.8 pKd = 6.8 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 143215 0 None - 1 Human 6.8 pKd = 6.8 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
3640 7556 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
In a calcium mobilisation assay using RBL-2H3 cells stably expressing the hC3aR.In a calcium mobilisation assay using RBL-2H3 cells stably expressing the hC3aR.
Guide to Pharmacology None None None None 9476119
3915 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 8307 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
8380 7055 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25446428
49799093 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5761 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1172879 8433 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
134813896 10431 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
60201789 10431 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
8379 10431 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
5776 10901 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3640 7556 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
8381 7816 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 25259874
91827354 7816 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 25259874
CHEMBL3342689 7816 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 25259874
71566654 7792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 24257095
9449 7792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 24257095
CHEMBL3736108 7792 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 24257095
3915 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
3915 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3915 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
49799079 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
49799079 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
5760 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
5760 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
91933514 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
91933514 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
CHEMBL1170024 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
CHEMBL1170024 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 8307 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
10595 8934 21 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.
Guide to Pharmacology 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 31910011
145996525 8934 21 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.
Guide to Pharmacology 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 31910011
CHEMBL4459627 8934 21 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.
Guide to Pharmacology 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 31910011
10224 7592 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26297549
10224 7592 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145417
25254550 7592 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26297549
25254550 7592 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145417
8384 7897 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 25259874
91827355 7897 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 25259874
CHEMBL3342676 7897 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 25259874
5777 8435 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3529 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 11342658
3529 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 33551801
5311120 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 11342658
5311120 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 33551801
CHEMBL389348 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 11342658
CHEMBL389348 10290 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 33551801
3915 8307 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 8307 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 8307 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 8307 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 8307 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893


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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
CHEMBL1170042 215327 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
155534696 178758 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 178758 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
3915 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
49799079 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
5760 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
91933514 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
8381 7816 3 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
91827354 7816 3 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL3342689 7816 3 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
3529 10290 9 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
5311120 10290 9 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL389348 10290 9 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
89570442 121750 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342686 121750 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
127035774 143215 0 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cellsDisplacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cells
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 143215 0 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cellsDisplacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cells
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
118716617 121741 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 121741 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
101886251 121743 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342679 121743 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
101886252 121747 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 121747 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
44430549 158045 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396030 158045 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
117634981 121746 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 121746 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
44430552 94780 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(C1CCCCC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234306 94780 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(C1CCCCC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430556 94826 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 431 6 1 3 4.6 O=C(NC1CCN(C(=O)/C=C/c2cccnc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234523 94826 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 431 6 1 3 4.6 O=C(NC1CCN(C(=O)/C=C/c2cccnc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430526 151013 1 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 CC1(C)CCC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL390464 151013 1 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 CC1(C)CCC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2007.04.023
44430559 94945 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 454 6 1 2 5.0 O=C(NC1CCN(C(=O)Cc2cccc(F)c2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234730 94945 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 454 6 1 2 5.0 O=C(NC1CCN(C(=O)Cc2cccc(F)c2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426471 92478 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228846 92478 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
117634952 143312 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 143312 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634952 143312 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 143312 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127034743 143311 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
CHEMBL3736489 143311 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
127034743 143311 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
CHEMBL3736489 143311 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
89570392 143255 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 143255 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570392 143255 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 143255 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570442 121750 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342686 121750 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
101886252 121747 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 121747 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
136110886 214781 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 389 6 1 2 4.5 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL97303 214781 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 389 6 1 2 4.5 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
89570147 121748 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342684 121748 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
101886254 121744 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 121744 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL1170026 215318 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
101886254 121744 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 121744 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
127036518 143153 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 143153 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127036518 143153 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 143153 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
3529 10290 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
5311120 10290 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL389348 10290 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL1170029 215321 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
44430538 94500 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 Cc1cc(C)cc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
CHEMBL233671 94500 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 Cc1cc(C)cc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
44426458 93066 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 358 8 5 4 1.7 Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL231303 93066 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 358 8 5 4 1.7 Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
136110890 214298 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 411 7 1 3 4.9 COc1ccc2c(c1)/C(=N/CCc1ccc(C)cc1)N=C2NCCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL94579 214298 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 411 7 1 3 4.9 COc1ccc2c(c1)/C(=N/CCc1ccc(C)cc1)N=C2NCCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
89570147 121748 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342684 121748 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
44430555 94825 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2ccc(F)nc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234522 94825 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2ccc(F)nc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430560 94946 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 448 6 1 2 5.3 O=C(NC1CCN(C(=O)/C=C/c2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234731 94946 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 448 6 1 2 5.3 O=C(NC1CCN(C(=O)/C=C/c2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430514 157021 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL395233 157021 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL1170026 215318 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
136110896 114501 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 390 6 1 3 3.9 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3cnccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL319113 114501 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 390 6 1 3 3.9 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3cnccc32)cc1 10.1016/s0960-894x(01)00522-4
71566653 143208 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 143208 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566653 143208 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 143208 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127034744 143184 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735339 143184 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
3529 10290 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
5311120 10290 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL389348 10290 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL1170029 215321 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565581 143126 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734765 143126 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565581 143126 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734765 143126 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44426496 148820 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL387755 148820 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
101886253 121742 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 121742 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
71565580 143262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 143262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565506 143254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 143254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565506 143254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 143254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170639 215349 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71565580 143262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 143262 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170639 215349 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71565509 143202 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735465 143202 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
101886253 121742 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 121742 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
71565509 143202 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735465 143202 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44430548 94731 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(F)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234101 94731 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(F)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426497 92510 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229006 92510 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1169838 215316 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44430510 165897 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
CHEMBL409773 165897 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
44426466 148812 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 8 5 4 2.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL387686 148812 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 8 5 4 2.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430553 94824 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ncccc1CCC(=O)N1CCC(NC(=O)C(c2ccccc2)C2CCCCC2)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL234521 94824 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ncccc1CCC(=O)N1CCC(NC(=O)C(c2ccccc2)C2CCCCC2)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL1169838 215316 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 215342 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 215342 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
135418443 114697 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 353 4 1 2 4.8 Cc1ccc(C/N=C2\N=C(NCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL319332 114697 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 353 4 1 2 4.8 Cc1ccc(C/N=C2\N=C(NCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
71566580 121749 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342685 121749 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
71768012 143230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 143230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566580 121749 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342685 121749 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
44430541 94501 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 467 7 1 3 5.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL233675 94501 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 467 7 1 3 5.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44431783 94715 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 4 4.5 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccsc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234005 94715 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 4 4.5 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccsc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426462 93168 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 369 8 5 5 1.3 N#Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL231404 93168 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 369 8 5 5 1.3 N#Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
44426464 103686 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 396 8 5 4 2.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccc(F)c(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL265866 103686 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 396 8 5 4 2.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccc(F)c(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426460 173109 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 10 5 5 1.8 CCOc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL427268 173109 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 10 5 5 1.8 CCOc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
44430546 94730 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1Cl)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234100 94730 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1Cl)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
44430558 158285 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 450 7 1 2 5.2 O=C(NC1CCN(C(=O)CCc2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396262 158285 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 450 7 1 2 5.2 O=C(NC1CCN(C(=O)CCc2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430516 93780 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 495 7 1 3 5.3 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL232418 93780 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 495 7 1 3 5.3 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.04.023
155534696 178758 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 178758 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
3915 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
49799079 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
5760 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
91933514 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 8307 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71768012 143230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 143230 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
3529 10290 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cellsDisplacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
5311120 10290 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cellsDisplacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
CHEMBL389348 10290 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cellsDisplacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
CHEMBL1170042 215327 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170644 215353 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170644 215353 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170230 215336 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170230 215336 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170025 215317 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170025 215317 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44430536 93529 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccccc1C(C(=O)NC1CCN(C(=O)CCc2cccnc2)CC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL232029 93529 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccccc1C(C(=O)NC1CCN(C(=O)CCc2cccnc2)CC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430529 94102 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 7 1 3 4.8 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)/C(=C/C1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL233232 94102 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 7 1 3 4.8 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)/C(=C/C1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
71566652 143316 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 143316 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566652 143316 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 143316 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170033 215324 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170046 215331 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170046 215331 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71566581 143282 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 143282 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
25156014 182228 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 182228 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
71566581 143282 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 143282 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
101886250 121753 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 121753 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
101886250 121753 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 121753 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
44430554 158048 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396031 158048 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426495 92509 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229005 92509 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
11252 7557 39 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 7557 39 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 7557 39 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430550 94778 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 478 8 1 5 4.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc([N+](=O)[O-])cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234304 94778 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 478 8 1 5 4.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc([N+](=O)[O-])cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426469 92454 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 400 8 5 5 2.6 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2csc3ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228634 92454 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 400 8 5 5 2.6 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2csc3ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426457 149655 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 362 8 5 4 1.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL389349 149655 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 362 8 5 4 1.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426459 156152 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 5 5 1.4 COc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL394538 156152 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 5 5 1.4 COc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
44430532 94104 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 417 7 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CC=CC1 10.1016/j.bmcl.2007.04.023
CHEMBL233234 94104 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 417 7 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CC=CC1 10.1016/j.bmcl.2007.04.023
CHEMBL1170033 215324 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
136110895 214571 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 410 5 2 3 4.8 CC(=O)Nc1ccc2c(c1)/C(=N\Cc1ccc(C)cc1)N=C2NCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL96138 214571 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 410 5 2 3 4.8 CC(=O)Nc1ccc2c(c1)/C(=N\Cc1ccc(C)cc1)N=C2NCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
44426470 92455 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 8 5 5 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc3c2oc2ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228635 92455 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 8 5 5 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc3c2oc2ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
25156014 182228 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 182228 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL1170638 215348 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170638 215348 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
127034742 143245 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735887 143245 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127034742 143245 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735887 143245 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
136110894 214802 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.2 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3cc(Cl)c(Cl)cc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL97420 214802 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.2 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3cc(Cl)c(Cl)cc32)cc1 10.1016/s0960-894x(01)00522-4
71525749 143207 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 143207 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71525749 143207 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 143207 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
24829327 172237 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assayDisplacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assay
ChEMBL 463 9 5 5 1.1 N=C(N)NCCC[C@H](NC(=O)c1cccn(Cc2ccccc2Br)c1=O)C(=O)O 10.1021/acs.jmedchem.7b00882
CHEMBL4239466 172237 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assayDisplacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assay
ChEMBL 463 9 5 5 1.1 N=C(N)NCCC[C@H](NC(=O)c1cccn(Cc2ccccc2Br)c1=O)C(=O)O 10.1021/acs.jmedchem.7b00882
17753143 92715 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 92715 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
101886249 121745 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 121745 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
44430547 175638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL438129 175638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
3529 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
3529 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.022
5311120 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.022
CHEMBL389348 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.022
11252 7557 39 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 7557 39 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 7557 39 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430557 94944 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 6 1 3 4.9 Cc1cncc(/C=C/C(=O)N2CCC(NC(=O)C(c3ccccc3)C3CCCCC3)CC2)c1 10.1016/j.bmcl.2007.04.023
CHEMBL234729 94944 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 6 1 3 4.9 Cc1cncc(/C=C/C(=O)N2CCC(NC(=O)C(c3ccccc3)C3CCCCC3)CC2)c1 10.1016/j.bmcl.2007.04.023
44426478 92492 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 452 9 5 4 1.8 N=C(N)NCCC[C@@H](NC(=O)N1CCN(C(c2ccccc2)c2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228900 92492 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 452 9 5 4 1.8 N=C(N)NCCC[C@@H](NC(=O)N1CCN(C(c2ccccc2)c2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2007.04.022
136110893 214294 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 476 10 1 4 4.5 CN(C)CCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL94544 214294 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 476 10 1 4 4.5 CN(C)CCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
101886249 121745 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 121745 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
71565510 143171 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 143171 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565582 143232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 143232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
3529 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 10290 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
17753143 92715 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 92715 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
71565510 143171 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 143171 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565582 143232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 143232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170030 215322 11 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
136110892 214744 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.7 CC(C/N=C1\N=C(NCC(C)c2ccc(Cl)cc2)c2ccccc21)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL97134 214744 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.7 CC(C/N=C1\N=C(NCC(C)c2ccc(Cl)cc2)c2ccccc21)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00522-4
136110887 214308 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 447 9 1 3 5.3 CCCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL94618 214308 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 447 9 1 3 5.3 CCCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
101886248 121752 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 121752 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
136110891 214148 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 381 6 1 2 4.9 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL93713 214148 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 381 6 1 2 4.9 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
17753143 92715 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL230034 92715 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430527 94029 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 469 7 1 3 4.7 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL233028 94029 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 469 7 1 3 4.7 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2007.04.023
44430539 94694 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL233879 94694 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL1170031 215323 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170030 215322 11 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170031 215323 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44426475 151447 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL390834 151447 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430528 94030 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 489 7 1 3 5.8 CC1(C)CC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC(C)(C)C1 10.1016/j.bmcl.2007.04.023
CHEMBL233029 94030 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 489 7 1 3 5.8 CC1(C)CC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC(C)(C)C1 10.1016/j.bmcl.2007.04.023
101886248 121752 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 121752 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
10595 8934 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
145996525 8934 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL4459627 8934 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
8384 7897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 7897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 7897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
117634949 143228 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735746 143228 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634949 143228 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735746 143228 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
136110889 112977 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1ccc(CC/N=C2\N=C(NCCc3ccc(Cl)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL313866 112977 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1ccc(CC/N=C2\N=C(NCCc3ccc(Cl)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL1170027 215319 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
136110897 214788 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1cccc(CC/N=C2\N=C(NCCc3cccc(Cl)c3)c3ccccc32)c1 10.1016/s0960-894x(01)00522-4
CHEMBL97335 214788 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1cccc(CC/N=C2\N=C(NCCc3cccc(Cl)c3)c3ccccc32)c1 10.1016/s0960-894x(01)00522-4
117634979 143133 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 143133 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634979 143133 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 143133 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570463 121751 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342687 121751 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
17753265 93530 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1cccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
CHEMBL232031 93530 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1cccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
44426463 93169 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL231405 93169 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170027 215319 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565508 143274 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736195 143274 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
11252 7557 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 7557 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 7557 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430530 94103 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 8 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(CC1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL233233 94103 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 8 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(CC1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
44430551 94779 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234305 94779 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430533 148878 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL388204 148878 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
44430531 159372 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 419 7 1 3 4.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL397190 159372 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 419 7 1 3 4.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.04.023
44426465 92447 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 392 8 5 4 2.4 Cc1ccc(Cl)cc1-c1ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o1 10.1016/j.bmcl.2007.04.022
CHEMBL228582 92447 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 392 8 5 4 2.4 Cc1ccc(Cl)cc1-c1ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o1 10.1016/j.bmcl.2007.04.022
44426472 92479 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228847 92479 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426481 92493 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 444 10 5 3 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228901 92493 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 444 10 5 3 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426461 156154 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 6 5 0.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(CO)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL394539 156154 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 6 5 0.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(CO)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170646 215354 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44430513 99137 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 5 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2007.04.023
CHEMBL243048 99137 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 5 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2007.04.023
10595 8934 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
145996525 8934 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL4459627 8934 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
8384 7897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 7897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 7897 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
71565508 143274 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736195 143274 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170637 215347 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170637 215347 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170646 215354 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
136110888 214639 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 325 4 1 2 4.1 CC(C)NC1=N/C(=N\CCc2ccc(Cl)cc2)c2ccccc21 10.1016/s0960-894x(01)00522-4
CHEMBL96477 214639 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 325 4 1 2 4.1 CC(C)NC1=N/C(=N\CCc2ccc(Cl)cc2)c2ccccc21 10.1016/s0960-894x(01)00522-4
89570463 121751 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342687 121751 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
117637102 143308 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 143308 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117637102 143308 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 143308 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566654 7792 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 7792 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 7792 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
71566654 7792 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 7792 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 7792 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
118716617 121741 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 121741 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
117634981 121746 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 121746 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
11252 7557 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.
Guide to Pharmacology 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 17459702
44430519 7557 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.
Guide to Pharmacology 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 17459702
CHEMBL390036 7557 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.
Guide to Pharmacology 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 17459702
11286 8378 0 None - 1 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 28562031