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 207417 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 206796 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 206799 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 206819 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 206806 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 212974 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 206799 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 206806 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 206814 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 206814 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 114463 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 114463 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 85294 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 85294 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 206787 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 206788 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 85293 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 85293 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 212886 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 114463 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 114463 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 206787 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 206788 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 212589 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 207426 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 164878 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 164878 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 85499 2 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 85499 2 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 87562 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 87562 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 206786 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 144124 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 144124 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 207418 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 135893 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 135893 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 135893 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 135893 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 212899 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 206786 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 206797 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 135916 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 135916 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 135916 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 135916 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 141498 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 141498 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 207416 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 150725 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 150725 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 168282 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 168282 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 206790 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 756 31 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 756 31 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 756 31 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 206794 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 206797 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 1011 1 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 1011 1 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 1011 1 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 206790 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 206794 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 207424 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 135941 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 135941 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 135941 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 135941 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 206785 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 206810 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 1011 1 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 1011 1 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 1011 1 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 207422 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 206810 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 206804 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 206785 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 206804 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 135968 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 135968 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 206821 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 207424 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 135968 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 135968 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 206821 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 213584 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 206824 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 206824 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 213296 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 206812 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 206812 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 206817 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 206795 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 206817 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 206817 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 206795 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 207420 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 207425 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 206820 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 206820 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 206825 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 212889 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 206816 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 206825 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 206816 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 213203 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 206791 9 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 206802 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 206803 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 114464 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 114464 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 1614 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 1614 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 1614 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 206791 9 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 206802 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 85263 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 85263 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 206803 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 114464 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 114464 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 135839 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 135839 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 135839 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 135839 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 1614 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 1614 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 1614 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 213038 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 213632 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 135870 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 135870 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 206813 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 206813 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 206811 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 206811 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 207423 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 206815 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 206815 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 135857 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 135857 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 136002 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 136002 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 85953 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 85953 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 135857 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 135857 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 136002 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 136002 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 206798 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 206837 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 206818 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 206807 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 206818 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 135998 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 135998 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 206807 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 135998 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 135998 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 206798 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 213088 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 135918 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 135918 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 135918 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 135918 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 206837 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 212757 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 212478 4 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 135894 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 135894 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 135894 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 135894 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 206789 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 207376 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 207376 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 206800 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 213172 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 206800 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 212957 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 207423 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 207425 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 207419 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 206808 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 206808 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 213586 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 988 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 988 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 988 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 988 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 988 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 988 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 988 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 988 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 988 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 135948 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 135948 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 212864 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 207421 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 135940 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 135940 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 206801 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 135940 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 135940 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 135819 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 135819 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 135819 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 135819 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 213592 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 206784 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 207422 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 150722 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 150722 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 206784 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 206801 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 135948 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 135948 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 207427 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 135994 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 135994 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 135994 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 135994 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 212687 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 206805 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 206805 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 206796 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 1090 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 1090 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 1090 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
3529 3448 8 None - 1 Human 8.9 pIC50 = 8.9 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 3448 8 None - 1 Human 8.9 pIC50 = 8.9 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 3448 8 None - 1 Human 8.9 pIC50 = 8.9 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
CHEMBL2064013 207419 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 2113 17 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 2113 17 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 2113 17 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 207418 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 170363 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 170363 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 171493 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 171493 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 174233 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 174233 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 114455 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 114455 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 114456 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 114456 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 207425 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 207427 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 114456 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 114456 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 171495 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 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 171495 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 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 173758 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 173758 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 3448 8 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 3448 8 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 3448 8 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 114455 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 114455 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 135901 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 135901 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 171495 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 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 171495 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 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 173758 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 173758 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 207424 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 85499 2 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 85499 2 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 114457 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 114457 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 170558 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 170558 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 85499 2 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 85499 2 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 114458 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 114458 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 169572 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 169572 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 114457 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 114457 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 170558 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 170558 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 114458 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 114458 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 169572 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 169572 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 207417 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 172933 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 172933 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 206822 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 173762 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 173762 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 172933 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 172933 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 173762 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 173762 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 207425 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 3448 8 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 3448 8 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 3448 8 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 114454 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 114454 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 169664 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 169664 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 169664 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 169664 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 174131 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 174131 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 174060 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 174060 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 171575 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 171575 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 174060 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 174060 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 149697 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 149697 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 165273 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 165273 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 171575 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 171575 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 174113 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 174113 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 114453 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 114453 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 114454 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 114454 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 3448 8 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 3448 8 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 3448 8 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 174689 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 174689 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 114453 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 114453 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 174131 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 174131 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 207423 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 174113 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 174113 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 174689 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 174689 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 207420 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 207416 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 175575 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 175575 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 175575 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 175575 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 114452 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 114452 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 170664 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 170664 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 170664 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 170664 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 171403 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 171403 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 169241 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 169241 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 171522 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 171522 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 207426 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 169241 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 169241 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 158560 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 158560 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 206789 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 114452 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 114452 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 171522 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 171522 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 171403 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 171403 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 207421 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 174866 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 174866 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 171362 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 171362 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 1090 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 1090 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 1090 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 171362 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 171362 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 174866 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 174866 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 207424 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 207422 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 170363 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 170363 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 135901 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 135901 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 135901 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 135901 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 753 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 1492 13 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 1492 13 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 1492 13 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 1492 13 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 1492 13 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
8380 265 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25446428
49799093 1614 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5761 1614 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1172879 1614 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
134813896 3589 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
60201789 3589 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
8379 3589 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
5776 4053 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3640 753 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
8381 1011 1 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 1011 1 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 1011 1 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 988 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 988 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 988 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 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
3915 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3915 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
49799079 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
49799079 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
5760 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
5760 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
91933514 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
91933514 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
CHEMBL1170024 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
CHEMBL1170024 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 1492 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
10595 2113 17 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 2113 17 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 2113 17 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 790 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26297549
10224 790 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145417
25254550 790 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26297549
25254550 790 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145417
8384 1090 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 1090 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 1090 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 1616 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3529 3448 8 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 1492 13 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 1492 13 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 1492 13 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 1492 13 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 1492 13 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 206796 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 171403 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 171403 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 1011 1 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 1011 1 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 1011 1 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 3448 8 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 3448 8 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 3448 8 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 114461 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 114461 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 135901 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 135901 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 114452 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 114452 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 114454 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 114454 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 114458 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 114458 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 150722 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 150722 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 114457 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 114457 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 87563 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 87563 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 87609 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 87609 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 143691 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 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 143691 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 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 87728 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 87728 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 85262 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 85262 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 135998 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 135998 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 135998 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 135998 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 135997 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 135997 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 135997 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 135997 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 135941 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 135941 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 135941 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 135941 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 114461 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 114461 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 114458 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 114458 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 206252 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 206252 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 114459 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 114459 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 114455 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 114455 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 206787 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 114455 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 114455 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 135839 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 135839 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 135839 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 135839 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 3448 8 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 3448 8 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 3448 8 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 206790 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 87283 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 87283 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 85850 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 85850 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 205776 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 205776 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 114459 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 114459 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 87608 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 87608 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 87729 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 87729 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 149697 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 149697 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 206787 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 107225 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 107225 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 135894 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 135894 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 135894 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 135894 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 135870 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 135870 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 3448 8 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 3448 8 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 3448 8 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 206790 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 135812 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 135812 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 135812 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 135812 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 141498 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 141498 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 114453 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 114453 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 135948 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 135948 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 135940 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 135940 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 135940 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 135940 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 206818 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 135948 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 135948 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 206818 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 135888 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 135888 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 114453 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 114453 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 135888 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 135888 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 87514 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 87514 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 85294 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 85294 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 206785 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 158560 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 158560 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 141490 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 141490 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 87607 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 87607 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 206785 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 206811 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 206811 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 107421 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 107421 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 114460 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 114460 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 135916 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 135916 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 114460 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 114460 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 87284 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 87284 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 87498 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 87498 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 85952 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 85952 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 96450 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 96450 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 165766 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 165766 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 87513 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 87513 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 150962 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 150962 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 86563 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 86563 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 171403 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 171403 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 1492 13 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 135916 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 135916 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 3448 8 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 3448 8 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 3448 8 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 206796 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 206822 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 206822 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 206805 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 206805 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 206786 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 206786 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 86313 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 86313 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 86885 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 86885 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 136002 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 136002 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 136002 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 136002 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 206793 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 206800 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 206800 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 135968 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 135968 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 174866 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 174866 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 135968 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 135968 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 114464 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 114464 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 114464 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 114464 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 150725 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 150725 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 85293 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 85293 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 756 31 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 756 31 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 756 31 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 87561 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 87561 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 85238 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 85238 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 142333 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 142333 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 148829 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 148829 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 86887 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 86887 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 206793 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 206047 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 206047 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 85239 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 85239 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 174866 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 174866 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 206817 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 206817 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 135931 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 135931 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 135931 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 135931 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 206273 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 206273 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 135893 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 135893 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 135893 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 135893 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 164895 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 164895 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 85499 2 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 85499 2 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 114456 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 114456 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 168282 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 168282 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 3448 8 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 756 31 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 756 31 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 756 31 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 87727 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 87727 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 85276 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 85276 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 205772 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 205772 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 114456 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 114456 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 135857 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 135857 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 135918 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 135918 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 3448 8 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 3448 8 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 3448 8 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 85499 2 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 85499 2 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 135857 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 135857 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 135918 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 135918 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 206791 9 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 206216 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 206216 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 205786 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 205786 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 114463 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 114463 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 205627 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 205627 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 85499 2 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 85499 2 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 86812 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 86812 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 87477 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 87477 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 206792 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 206791 9 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 206792 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 144124 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 144124 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 86813 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 86813 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 114463 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 114463 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 2113 17 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 2113 17 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 2113 17 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 1090 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 1090 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 1090 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 135914 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 135914 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 135914 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 135914 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 105706 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 105706 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 206788 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 206259 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 206259 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 135819 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 135819 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 135819 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 135819 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 114462 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 114462 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 86314 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 86314 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 85953 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 85953 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 206788 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 135960 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 135960 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 756 31 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 756 31 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 756 31 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 86886 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 86886 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 87562 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 87562 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 141556 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 141556 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 152049 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 152049 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 85231 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 85231 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 85263 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 85263 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 85277 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 85277 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 148831 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 148831 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 206823 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 91916 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 91916 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 2113 17 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 2113 17 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 2113 17 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 1090 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 1090 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 1090 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 135960 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 135960 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 206816 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 206816 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 206823 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 206114 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 206114 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 114462 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 114462 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 135994 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 135994 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 135994 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 135994 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 988 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 988 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 988 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 988 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 988 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 988 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 114452 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 114452 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 114457 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 114457 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 756 31 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 756 31 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 756 31 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 1561 0 None - 1 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 28562031