Ligand source activities (1 row/activity)





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155491018 174083 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
10585 1079 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 174083 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 1 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
10585 1079 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 174083 1 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 174083 1 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 10 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
44453327 95095 25 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL255408 95095 25 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
10585 1079 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1079 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 174083 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 174083 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 174083 1 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 3 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
69212799 77976 3 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL2096789 77976 3 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 439 6 2 3 3.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
508750 168535 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
CHEMBL435499 168535 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 467 7 2 3 4.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NCC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2004.08.009
10585 1079 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as pEC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.10 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1079 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1079 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1079 1 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)Non-competitive insurmountable antagonist activity at human CCR2 expressed in human U2OS cell membranes assessed as EC50 for CCL2-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
44395055 64504 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
CHEMBL181432 64504 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 6 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CCCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2004.08.009
73351183 93234 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2448120 93234 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
70697571 77975 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
CHEMBL2096788 77975 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Inhibition of MCP-1 induced chemotaxis in THP-1 cellsInhibition of MCP-1 induced chemotaxis in THP-1 cells
ChEMBL 453 7 2 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC[C@H]1CCCN1Cc1ccc(Cl)cc1 10.1016/j.bmcl.2004.08.009
11735999 189350 0 None - 1 Human 10.4 pED50 = 10.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 212 1 2 2 0.8 CC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL512607 189350 0 None - 1 Human 10.4 pED50 = 10.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 212 1 2 2 0.8 CC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11322108 178567 0 None - 1 Human 10.2 pED50 = 10.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 226 3 2 2 1.2 CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL467070 178567 0 None - 1 Human 10.2 pED50 = 10.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 226 3 2 2 1.2 CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11254190 189352 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 268 5 2 2 2.2 CC(C)CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL512615 189352 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 268 5 2 2 2.2 CC(C)CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11651747 173769 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 252 2 2 2 1.7 CC1(C(=O)N[C@H]2CCCCNC2=O)CCCCC1 10.1021/jm900133w
CHEMBL453720 173769 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 252 2 2 2 1.7 CC1(C(=O)N[C@H]2CCCCNC2=O)CCCCC1 10.1021/jm900133w
11659300 178764 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
CHEMBL468733 178764 0 None - 0 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
11151928 189487 0 None 1 4 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL513863 189487 0 None 1 4 Human 10.1 pED50 = 10.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11173161 188807 0 None - 1 Human 9.7 pED50 = 9.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 266 4 2 2 2.2 CC(C)=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL506023 188807 0 None - 1 Human 9.7 pED50 = 9.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 266 4 2 2 2.2 CC(C)=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157844 189289 0 None - 1 Human 9.4 pED50 = 9.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
CHEMBL512094 189289 0 None - 1 Human 9.4 pED50 = 9.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 290 2 2 2 2.0 O=C1NCCCC[C@H]1NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm900133w
11218678 170353 0 None - 1 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 240 4 2 2 1.6 CCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL444736 170353 0 None - 1 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 240 4 2 2 1.6 CCCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11543222 193507 3 None - 1 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 2 2 2 1.4 O=C(N[C@H]1CCCCNC1=O)C1CCCCC1 10.1021/jm900133w
CHEMBL526704 193507 3 None - 1 Human 9.3 pED50 = 9.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 2 2 2 1.4 O=C(N[C@H]1CCCCNC1=O)C1CCCCC1 10.1021/jm900133w
11536008 178594 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 236 2 2 2 1.3 O=C(N[C@H]1CCCCNC1=O)C1=CCCCC1 10.1021/jm900133w
CHEMBL467276 178594 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 236 2 2 2 1.3 O=C(N[C@H]1CCCCNC1=O)C1=CCCCC1 10.1021/jm900133w
11551248 178660 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 304 3 2 2 2.4 O=C(CC12CC3CC(CC(C3)C1)C2)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL467685 178660 0 None - 0 Human 9.1 pED50 = 9.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 304 3 2 2 2.4 O=C(CC12CC3CC(CC(C3)C1)C2)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11390777 172616 0 None - 0 Human 9.0 pED50 = 9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 4 2 2 1.4 C=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL449215 172616 0 None - 0 Human 9.0 pED50 = 9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 238 4 2 2 1.4 C=CCC(C)(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11198073 178479 0 None - 1 Human 8.0 pED50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 322 10 2 2 3.9 CCCCCCCCC/C=C(\C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466434 178479 0 None - 1 Human 8.0 pED50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 322 10 2 2 3.9 CCCCCCCCC/C=C(\C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11370332 63296 0 None - 1 Human 7.8 pED50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 310 11 2 2 3.7 CCCCCCCCCCCC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL179312 63296 0 None - 1 Human 7.8 pED50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 310 11 2 2 3.7 CCCCCCCCCCCC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157843 178477 0 None - 1 Human 6.7 pED50 = 6.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466432 178477 0 None - 1 Human 6.7 pED50 = 6.7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44157843 178477 0 None - 1 Human 8.5 pED50 = 8.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL466432 178477 0 None - 1 Human 8.5 pED50 = 8.5 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 324 11 2 2 3.9 CCCCCCCCCCC(C)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11151929 178763 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCC(C)(C)CC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL468732 178763 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCC(C)(C)CC(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
11359715 178762 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL468720 178762 0 None - 0 Human 8.4 pED50 = 8.4 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 338 11 2 2 4.3 CCCCCCCCCCC(C)(C)C(=O)N[C@@H]1CCCCNC1=O 10.1021/jm900133w
11544064 178478 0 None - 1 Human 8.3 pED50 = 8.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 308 6 2 2 3.2 CCCCCC1CCC(C(=O)N[C@H]2CCCCNC2=O)CC1 10.1021/jm900133w
CHEMBL466433 178478 0 None - 1 Human 8.3 pED50 = 8.3 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 308 6 2 2 3.2 CCCCCC1CCC(C(=O)N[C@H]2CCCCNC2=O)CC1 10.1021/jm900133w
11609693 189212 0 None - 0 Human 8.2 pED50 = 8.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 334 6 2 2 3.7 CCCCCC12CCC(C(=O)N[C@H]3CCCCNC3=O)(CC1)CC2 10.1021/jm900133w
CHEMBL511426 189212 0 None - 0 Human 8.2 pED50 = 8.2 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 334 6 2 2 3.7 CCCCCC12CCC(C(=O)N[C@H]3CCCCNC3=O)(CC1)CC2 10.1021/jm900133w
11437477 188624 0 None - 1 Human 8.1 pED50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 280 4 2 2 1.3 CC(CCl)(CCl)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
CHEMBL502976 188624 0 None - 1 Human 8.1 pED50 = 8.1 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assayAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis after 2 hrs by microtiter format trans-well migration assay
ChEMBL 280 4 2 2 1.3 CC(CCl)(CCl)C(=O)N[C@H]1CCCCNC1=O 10.1021/jm900133w
44593562 187495 0 None - 1 Human 10.0 pIC50 = 10 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187495 0 None - 1 Human 10.0 pIC50 = 10 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
86642531 138303 0 None 10 2 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770912 138303 0 None 10 2 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
44425645 86082 0 None 7 2 Human 9.8 pIC50 = 9.8 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86082 0 None 7 2 Human 9.8 pIC50 = 9.8 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
10240064 188428 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 188428 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593562 187495 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187495 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
44425652 168768 0 None 12 2 Human 9.6 pIC50 = 9.6 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168768 0 None 12 2 Human 9.6 pIC50 = 9.6 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
10289827 187976 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL497202 187976 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 571 9 2 6 3.8 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44593563 193110 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL522688 193110 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 508 7 2 3 5.9 CCC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
44425647 86101 0 None 5 2 Human 9.5 pIC50 = 9.5 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL231039 86101 0 None 5 2 Human 9.5 pIC50 = 9.5 Functional
Inhibition of chemotaxis in human MCP1 monocytesInhibition of chemotaxis in human MCP1 monocytes
ChEMBL 542 6 1 2 7.4 CC(C)C[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
44425292 85968 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230281 85968 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425292 85968 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230281 85968 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
10240064 188428 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502247 188428 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 10 2 6 4.6 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
46865775 8114 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091605 8114 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 579 8 1 5 4.4 CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
24801689 97794 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
CHEMBL271828 97794 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 651 9 5 6 3.5 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)C2CCCCC2)cc1 10.1021/jm701488f
44425255 168884 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL438304 168884 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 650 8 2 5 7.2 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)[C@@H](C)C2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425652 168768 0 None 12 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
CHEMBL437359 168768 0 None 12 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2007.04.053
59370257 138164 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 2 2 6 1.9 Cc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769444 138164 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 2 2 6 1.9 Cc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
10129192 188459 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL502793 188459 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 599 11 2 6 4.6 CCN(CC)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
11598 673 9 None 812 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
23725177 673 9 None 812 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4442783 673 9 None 812 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 6 2 6 3.4 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C 10.1021/acsmedchemlett.1c00373
44425254 142260 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL388487 142260 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 636 8 2 5 7.0 CC(=O)Nc1nc(C(CCN2CCC3(C=Cc4ccccc43)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 153529 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL397996 153529 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
44425645 86082 0 None 7 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
CHEMBL230933 86082 0 None 7 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of Ca2+ flux in human monocytesInhibition of Ca2+ flux in human monocytes
ChEMBL 528 5 1 2 7.0 CC(C)[C@]1(C(=O)NCc2cc(F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2007.04.053
11597 674 5 None 11 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
23725180 674 5 None 11 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
CHEMBL4781426 674 5 None 11 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 506 5 3 6 3.5 CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C 10.1021/acsmedchemlett.1c00373
51039119 176217 33 None -1 3 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
CHEMBL4594419 176217 33 None -1 3 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP-1 cells assessed as reduction in CCL2-induced chemotaxis
ChEMBL 484 5 3 8 2.2 CC(=O)N[C@@H]1C[C@H](NC(C)(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3cc(C(C)(C)C)nn23)C1=O 10.1021/acsmedchemlett.1c00373
44593564 187232 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187232 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
25022597 95339 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
CHEMBL256629 95339 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 6 3 4 3.0 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)c(C)c1 10.1016/j.bmcl.2008.02.015
44453440 97688 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL271288 97688 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 448 7 3 4 3.0 CCc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
183790 3742 11 None -1 5 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
783 3742 11 None -1 5 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
CHEMBL1178786 3742 11 None -1 5 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2015.02.019
183790 3742 11 None -1 5 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3742 11 None -1 5 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3742 11 None -1 5 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
24801690 98041 25 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 98041 25 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
57402219 71008 0 None 52 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71008 0 None 52 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
24801690 98041 25 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98041 25 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44593564 187232 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492564 187232 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 498 6 2 3 5.3 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2F)C1 10.1016/j.bmcl.2008.12.050
44573649 187235 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
CHEMBL492569 187235 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 548 6 2 3 6.1 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](NC2CCOCC2C(F)(F)F)C1 10.1016/j.bmcl.2008.12.050
44593562 187495 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
CHEMBL494191 187495 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assayAntagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
ChEMBL 494 6 2 3 5.6 CC1COCCC1N[C@@H]1CC[C@@](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)C1 10.1016/j.bmcl.2008.12.050
10175425 193533 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL526752 193533 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 614 10 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](N(C)C(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2009.05.041
127025088 138263 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 420 3 2 6 1.8 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C4CC4)cs3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770530 138263 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 420 3 2 6 1.8 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C4CC4)cs3)CC2)C1 10.1039/C5MD00362H
127025086 138183 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 442 4 2 6 2.3 CC(C)c1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769610 138183 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 442 4 2 6 2.3 CC(C)c1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
46865774 8113 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1091604 8113 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.1 M bovine serum albumin
ChEMBL 553 9 2 5 3.9 CC(C)N(C)[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
86642531 138303 0 None -10 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium fluxAntagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium flux
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
CHEMBL3770912 138303 0 None -10 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium fluxAntagonist activity at rat C-C chemokine receptor type 2 assessed as inhibition of CCL2-induced calcium flux
ChEMBL 482 2 2 6 2.6 CC(C)(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3nc(C(F)(F)F)c(Cl)s3)CC2)C1 10.1039/C5MD00362H
10007642 19109 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19109 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
10218403 187910 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
CHEMBL496630 187910 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 557 9 3 6 3.5 CN[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)[C@H](CS(=O)(=O)c2ccc(SC)cc2)C1 10.1016/j.bmcl.2009.05.041
46886055 8044 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albumin
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
CHEMBL1090893 8044 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albuminAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 45 mins in presence of 0.5 M bovine serum albumin
ChEMBL 593 9 1 5 4.8 CCN(C(C)C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(F)(F)F)c3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2010.03.035
127025093 138214 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 4 2 6 1.7 CCc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
CHEMBL3769984 138214 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assayAntagonist activity at human C-C chemokine receptor type 2 expressed in THP-1 cells assessed as inhibition of CCL2-induced calcium flux preincubated for 10 mins followed by CCL2 addition by Fluo-4 dye based FLIPR assay
ChEMBL 428 4 2 6 1.7 CCc1nc(NC(=O)N2CCN(C(=O)[C@H]3CN(C(C)C)CCN3)CC2)sc1Cl 10.1039/C5MD00362H
46830335 8215 8 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092238 8215 8 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 565 8 2 5 2.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
11365166 74544 1 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
CHEMBL2029423 74544 1 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 573 7 3 7 4.0 O=C(NCC(=O)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4nccs4)cn3)CC2)C1)c1cccc(C(F)(F)F)c1 10.1021/ml200199c
52941377 19329 0 None 7 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19329 0 None 7 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
16216716 153529 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397996 153529 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425292 85968 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
CHEMBL230281 85968 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2Inhibition of MCP1-stimulated chemotaxis in monocytes transfected with human CCR2
ChEMBL 627 9 3 5 6.6 CNC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2006.10.059
16216716 153529 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397996 153529 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 612 9 2 5 6.8 CC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
11353855 74549 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74549 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
44425652 168768 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL437359 168768 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425652 168768 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL437359 168768 0 None 12 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 526 5 1 2 6.7 C[C@H]1CN([C@@H]2CC[C@@](C(=O)NCc3cc(F)cc(C(F)(F)F)c3)(C3CC3)C2)CC[C@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
57335017 70338 0 None 1380 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
CHEMBL1944776 70338 0 None 1380 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSAAntagonist activity at CCR2 by monocyte transmigration assay in pesence of 0.5% BSA
ChEMBL 595 8 4 6 2.8 N[C@@H]1CC[C@H](NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)C[C@@H]1CS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.12.057
70691785 73727 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018391 73727 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 606 12 6 6 2.9 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCNCC1 10.1016/j.bmcl.2012.03.007
46830336 7850 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1089793 7850 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 567 8 2 5 2.4 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
54754967 77830 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL2092884 77830 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 518 7 4 7 3.0 COc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
10239991 188447 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL502516 188447 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 585 10 3 6 4.3 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NC(C)C)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
57391766 71017 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
CHEMBL1951776 71017 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 491 6 3 6 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN([C@H]2CC[C@@](O)(c3cnccn3)CC2)C1 10.1021/ml200030q
10187492 147790 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL393267 147790 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 549 11 5 5 3.7 CCNc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)N[C@@H](CNCc1ccc(C)cc1C)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
25256791 187691 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
CHEMBL495202 187691 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet stainingAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 1 hr by crystal violet staining
ChEMBL 494 6 2 3 5.6 CC(C)[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N[C@H]2CCOC[C@H]2C)C1 10.1016/j.bmcl.2010.02.072
11502371 153128 3 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 153128 3 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in PBMC assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
11502371 153128 3 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
CHEMBL397647 153128 3 None 22 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilizationAntagonist activity at CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced calcium mobilization
ChEMBL 407 5 1 2 5.0 C[N+](C)(Cc1ccc(NC(=O)c2ccc(Cl)c(Cl)c2)cc1)C1CCOCC1 10.1016/j.bmcl.2007.01.115
10154434 58789 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 342 4 2 5 3.2 CC(C)Oc1cccc(NC(=O)NC(=O)c2ccc3c(c2)OCO3)c1 10.1021/jm1012903
CHEMBL1687955 58789 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 342 4 2 5 3.2 CC(C)Oc1cccc(NC(=O)NC(=O)c2ccc3c(c2)OCO3)c1 10.1021/jm1012903
44413167 79719 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
CHEMBL211560 79719 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 447 8 2 3 4.2 CN(C)CCN[C@H](C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1ccccc1 10.1016/j.bmcl.2008.01.023
9967878 85079 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 342 4 2 3 3.9 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1F 10.1016/j.bmc.2006.09.052
CHEMBL224510 85079 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 342 4 2 3 3.9 Fc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1F 10.1016/j.bmc.2006.09.052
44421867 85157 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1cc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cs1 10.1016/j.bmc.2006.09.052
CHEMBL225166 85157 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 312 4 2 4 3.7 c1cc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cs1 10.1016/j.bmc.2006.09.052
44421889 85219 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCCC(Oc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225582 85219 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 307 4 1 3 3.6 c1ccc(CN2CCCC(Oc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098519 85230 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 336 5 2 4 3.6 COc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL225637 85230 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 336 5 2 4 3.6 COc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098523 142289 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 320 4 2 3 3.9 Cc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL388516 142289 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 320 4 2 3 3.9 Cc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421913 161884 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 334 4 2 3 3.4 O=C(Nc1ccc2[nH]ncc2c1)C1CCCN(Cc2ccccc2)C1 10.1016/j.bmc.2006.09.052
CHEMBL415061 161884 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 334 4 2 3 3.4 O=C(Nc1ccc2[nH]ncc2c1)C1CCCN(Cc2ccccc2)C1 10.1016/j.bmc.2006.09.052
21098488 166267 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL426925 166267 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 340 4 2 3 4.3 Clc1ccc(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
21098490 166325 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL427245 166325 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 326 4 2 3 3.9 Clc1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
44421917 166327 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
CHEMBL427254 166327 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 321 4 3 4 3.2 Nc1ccccc1CN1CCCC(Nc2ccc3[nH]ncc3c2)C1 10.1016/j.bmc.2006.09.052
9840006 142026 5 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL387625 142026 5 None - 1 Human 6.0 pIC50 = 6 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1cccc(CN2CC[C@@H](Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
9956238 60198 1 None -79 4 Rat 5.0 pIC50 = 5 Functional
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60198 1 None -79 4 Rat 5.0 pIC50 = 5 Functional
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60198 1 None -79 4 Rat 5.0 pIC50 = 5 Functional
Antagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in rat spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
44453002 155373 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 7 2 3 3.9 O=C(CCNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL403424 155373 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 453 7 2 3 3.9 O=C(CCNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1 10.1016/j.bmcl.2008.02.015
44421860 85048 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 295 4 3 3 3.0 c1c[nH]c(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
CHEMBL224166 85048 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 295 4 3 3 3.0 c1c[nH]c(CN2CCCC(Nc3ccc4[nH]ncc4c3)C2)c1 10.1016/j.bmc.2006.09.052
9900683 141912 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 292 4 2 3 3.2 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
CHEMBL386937 141912 0 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assayInhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay
ChEMBL 292 4 2 3 3.2 c1ccc(CN2CCC(Nc3ccc4[nH]ncc4c3)C2)cc1 10.1016/j.bmc.2006.09.052
10065796 142067 4 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 339 4 1 3 4.2 Fc1cccc(F)c1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL387954 142067 4 None - 1 Human 5.0 pIC50 = 5 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 339 4 1 3 4.2 Fc1cccc(F)c1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
54585109 62573 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782579 62573 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 468 5 1 5 3.7 CC(C)[C@]1(C(=O)N2CCN(c3cc(C(F)(F)F)ccn3)CC2)CC[C@@H](NC2CCOCC2)C1 10.1016/j.bmcl.2011.01.034
44453234 97471 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL270182 97471 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 489 7 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1 10.1016/j.bmcl.2008.02.015
22143196 183987 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL481790 183987 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.07.123
22143196 183987 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481790 183987 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 509 7 5 6 2.0 CSc1ccc(C(=O)NC2CCNCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
44416138 138874 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
CHEMBL378195 138874 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at CCR2b by calcium flux based FLIPR assay in CHO cellsActivity at CCR2b by calcium flux based FLIPR assay in CHO cells
ChEMBL 564 7 1 2 7.5 C[C@H]1CN(CC[C@H](C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2006.07.011
46927117 65428 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829619 65428 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1ccc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1016/j.bmcl.2011.06.080
44453405 95436 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
CHEMBL257062 95436 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 469 6 4 5 2.6 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1Cl 10.1016/j.bmcl.2008.02.015
44453407 95437 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257063 95437 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 450 7 3 5 2.4 COc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1 10.1016/j.bmcl.2008.02.015
56675205 65795 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834788 65795 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 3 5 4.2 Cc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4n[nH]c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
56671793 65796 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834789 65796 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 486 6 2 6 3.9 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cccnc4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
56671795 65799 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834792 65799 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 478 6 3 6 4.0 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](c3cncs3)CC2)C1 10.1016/j.bmcl.2011.08.074
46884856 8344 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092921 8344 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 566 8 2 4 3.8 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cc(F)ccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
44583280 172449 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL447937 172449 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 640 9 3 6 4.9 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCCC2)cc1 10.1016/j.bmcl.2009.05.041
46885159 8375 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
CHEMBL1093153 8375 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1016/j.bmcl.2010.02.072
46885160 8376 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093154 8376 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccc(F)cc3)CC2)C1 10.1016/j.bmcl.2010.02.072
9974356 137591 4 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL375556 137591 4 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
57396726 68955 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 562 8 3 5 4.0 CS(=O)(=O)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
CHEMBL1922817 68955 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 562 8 3 5 4.0 CS(=O)(=O)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
44439163 90294 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL238518 90294 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 596 12 4 7 4.7 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
183790 3742 11 None -1 5 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
783 3742 11 None -1 5 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
CHEMBL1178786 3742 11 None -1 5 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.bmc.2018.05.027
11283842 73738 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018402 73738 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 522 13 5 5 4.5 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(NCC)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
11353855 74549 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
CHEMBL2029568 74549 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometryAntagonist activity at CCR2 receptor in human whole blood assessed as inhibition of alexa-tagged MCP-induced effect 30 mins by flow cytometry
ChEMBL 595 6 2 8 4.2 O=C(C1CCN(c2cc(C(F)(F)F)ccn2)CC1)N1CC[C@H](N[C@H]2CC[C@@](O)(c3ccc(-c4ncccn4)cn3)CC2)C1 10.1021/ml200199c
56643545 68960 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68960 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
52943756 19290 0 None 23 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
CHEMBL1290412 19290 0 None 23 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at human CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 489 6 3 4 3.3 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1O 10.1016/j.bmcl.2010.10.020
44453368 97767 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
CHEMBL271725 97767 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 449 6 4 5 2.3 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)cc1N 10.1016/j.bmcl.2008.02.015
56683116 65806 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
CHEMBL1834799 65806 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 534 7 2 7 5.1 CC(C)c1ncc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)s1 10.1016/j.bmcl.2011.08.074
46884898 7717 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1088874 7717 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 564 8 2 4 4.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3ccccc3Cl)CC2)C1 10.1016/j.bmcl.2010.02.072
44453409 95439 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
CHEMBL257065 95439 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccc(CN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)cc1 10.1016/j.bmcl.2008.02.015
22143146 183906 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481202 183906 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 490 8 3 4 3.5 Cc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
10218843 172786 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL451340 172786 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 633 11 3 6 5.1 CSc1ccc(S(=O)(=O)C[C@@H]2C[C@H](NCc3ccccc3)CC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2009.05.041
44425641 86066 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230832 86066 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
10007642 19109 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1289203 19109 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 547 8 3 5 3.8 CCO[C@H]1CN([C@H]2CC[C@@](O)(c3ccc(C)cc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
46885028 8422 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
CHEMBL1093470 8422 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1ccccc1C(=O)N1CCN(CCN2CC[C@@H](NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2010.02.072
24801523 97855 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL272168 97855 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 493 7 3 4 4.0 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
57656833 75229 0 None -257 4 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036782 75229 0 None -257 4 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at mouse CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 427 3 2 4 2.4 CC(C)N1CCN[C@@H](C(=O)N2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
122181148 121836 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 478 6 1 3 5.2 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589843 121836 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 478 6 1 3 5.2 CC1Cc2ccccc2C2(CCN(CCCC(=O)NCc3cc(F)cc(C(F)(F)F)c3)CC2)O1 10.1016/j.bmc.2015.02.019
9956238 60198 1 None -95 4 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1688889 60198 1 None -95 4 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
CHEMBL1739922 60198 1 None -95 4 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 467 8 2 8 3.0 Cc1nn(C)c2nc(N(C)CCN(C)C)c(C(=O)NC(=O)Nc3cccc(OC(C)C)c3)cc12 10.1021/jm1012903
508742 95576 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL257702 95576 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 423 6 2 3 3.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(Cc2ccc(F)cc2)C1 10.1016/j.bmcl.2008.02.015
145963552 161348 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 489 6 1 5 4.1 CC(=O)N1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4125866 161348 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 489 6 1 5 4.1 CC(=O)N1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
122181146 121834 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589841 121834 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 544 7 1 4 5.7 COc1ccc2c(c1)CCOC21CCN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2015.02.019
44447435 94696 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252815 94696 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
44447435 94696 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
CHEMBL252815 94696 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 514 9 1 2 7.0 CCCC(CCN1CCC(c2ccccc2)CC1)C(=O)NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2008.01.023
145962429 161569 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 446 6 1 4 5.4 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCCCC1 10.1016/j.bmc.2018.05.027
CHEMBL4128975 161569 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 446 6 1 4 5.4 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCCCC1 10.1016/j.bmc.2018.05.027
44453538 97930 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
CHEMBL272543 97930 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 419 6 2 3 3.1 Cc1ccccc1CN1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2008.02.015
46240482 83577 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
CHEMBL2204259 83577 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 482 6 3 6 2.5 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@](O)(c3nccs3)CC2)C1 10.1021/ml300260s
22143294 193426 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526091 193426 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
44580590 193571 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 193571 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
70683350 73726 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
CHEMBL2018390 73726 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 607 12 5 6 3.4 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)N1CCOCC1 10.1016/j.bmcl.2012.03.007
44425641 86066 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL230832 86066 0 None 5 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 596 6 1 3 7.5 CSC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44425288 86015 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230507 86015 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425304 143367 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL389773 143367 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
69035677 77649 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
CHEMBL2088389 77649 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albuminAntagonist activity at CCR2 in human monocytes by chemotaxis assay in presence of 0.5% bovine serum albumin
ChEMBL 590 8 1 5 5.6 CCN(C(C)C)[C@@H]1CC[C@H](N2CCC(c3nc4cccc(C(F)(F)F)c4[nH]3)C2=O)[C@H](CS(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.08.002
44425288 86015 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL230507 86015 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 570 8 2 5 6.4 Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425304 143367 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL389773 143367 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44571218 183878 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL481009 183878 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 523 7 5 6 2.5 CSc1ccc(C(=O)NC2CC(N)CCC2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)cc1 10.1016/j.bmcl.2008.12.062
57344310 68936 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922794 68936 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 539 7 3 4 4.4 NC(=O)C(NC1CCC(c2c[nH]c3ncccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57343820 68954 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922816 68954 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 518 7 3 3 5.2 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2011.09.113
24801525 97609 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
CHEMBL270906 97609 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 526 7 4 5 1.9 NS(=O)(=O)c1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1021/jm701488f
49763686 65424 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829615 65424 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 7 3 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(C(=O)O)cc3)CC2)C1 10.1016/j.bmcl.2011.06.080
57396724 68947 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 485 7 2 3 4.1 NC(=O)C(NC1CCC(c2ccccc2)C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922805 68947 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 485 7 2 3 4.1 NC(=O)C(NC1CCC(c2ccccc2)C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57396725 68949 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 498 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)C2CC2c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922808 68949 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 498 7 3 3 4.7 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)C2CC2c2ccccc2)CC1 10.1016/j.bmcl.2011.09.113
44563039 192045 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 482 5 1 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL520228 192045 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 482 5 1 3 5.1 O=C(/C=C/c1cc(F)c(F)c(F)c1)N1CCC(CN2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
11179439 73736 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
CHEMBL2018400 73736 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 494 11 5 5 3.7 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CC(=O)Nc1cc(N)cc(C(F)(F)F)c1 10.1016/j.bmcl.2012.03.007
46947816 65433 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829624 65433 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 476 6 3 5 3.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@H](c3ccc(O)cn3)CC2)C1 10.1016/j.bmcl.2011.06.080
44563113 174583 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 515 5 3 4 5.4 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL455682 174583 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 515 5 3 4 5.4 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCC(C(CO)N2CCC(c3c[nH]c4ncccc34)CC2)CC1 10.1016/j.bmcl.2008.10.061
508877 95061 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL255209 95061 1 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 466 7 4 6 2.1 COc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
54756045 65788 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834781 65788 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 510 7 3 8 2.3 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3nn(C(N)=O)c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56678507 65800 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834793 65800 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4cncs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44447429 94643 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252412 94643 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
50925394 19328 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290636 19328 0 None -2 2 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 517 8 2 4 4.4 CCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
44447429 94643 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL252412 94643 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 550 7 1 2 7.1 C[C@H]1CN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CC2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
44425286 153247 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397750 153247 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
44425286 153247 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
CHEMBL397750 153247 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 670 9 2 6 8.2 CC(C)(C)OC(=O)Nc1nc([C@H](CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1 10.1016/j.bmcl.2008.01.023
57344299 68956 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922818 68956 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 552 7 3 3 5.6 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2011.09.113
56669631 65809 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
CHEMBL1834851 65809 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 489 6 2 7 3.3 Cn1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)n1 10.1016/j.bmcl.2011.08.074
132572938 156789 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
CHEMBL4070869 156789 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assayAntagonist activity at human CCR2b expressed in human Chem1 cells assessed as inhibition of human recombinant CCL2 induced Ca2+ mobilization preincubated for 10 mins followed by CCL2 induction measured every sec for 120 secs by Fluo-4-AM dye-based fluorescence assay
ChEMBL 551 8 1 4 6.4 Cc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc(CN(C)C4CCOCC4)cc2)CN(CC(C)C)C3=O)cc1 10.1016/j.ejmech.2017.04.046
44439158 146827 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
CHEMBL392493 146827 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 542 10 1 4 7.5 O=C(CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1)NCCCc1ccncc1 10.1016/j.bmcl.2006.10.060
10272003 58879 1 None -2 3 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
CHEMBL1688888 58879 1 None -2 3 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in mouse spleen cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 395 2 2 5 3.4 Cc1nn(C)c2ncc(C(=O)NC(=O)Nc3ccc(F)c(C(F)(F)F)c3)cc12 10.1021/jm1012903
57403700 68945 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.0 NC(=O)C(NC1Cc2ccccc2C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922803 68945 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 457 6 2 3 3.0 NC(=O)C(NC1Cc2ccccc2C1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
10427217 84997 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
CHEMBL223815 84997 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1cccc(CN2CCC(Nc3cccc4cnccc34)C2)c1 10.1016/j.bmc.2006.10.028
10041590 142111 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL388285 142111 4 None - 1 Human 4.9 pIC50 = 4.9 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
54584164 62568 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782574 62568 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nc(C(F)(F)F)cs3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
44595711 137321 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium fluxAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium flux
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
CHEMBL3752627 137321 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium fluxAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced inhibition of calcium flux
ChEMBL 332 2 1 1 5.1 C[C@H]1CC=C(C(=O)O)[C@](C)(c2ccc(Cl)c(C(F)(F)F)c2)C1 10.1016/j.bmcl.2015.11.051
49763568 65415 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829605 65415 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 503 6 2 5 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@@H](c3ccc4c(c3)OCO4)CC2)C1 10.1016/j.bmcl.2011.06.080
11752457 74539 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
CHEMBL2029417 74539 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 504 6 3 5 3.2 Cc1ccc([C@]2(O)CC[C@H](N[C@H]3CCN(C(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)nc1 10.1021/ml200199c
54755081 65777 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
CHEMBL1834719 65777 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 467 7 3 6 2.9 CCOC(=O)[C@H]1CC[C@@H](N2CC(NC(=O)CNc3n[nH]c4ccc(C(F)(F)F)cc34)C2)CC1 10.1016/j.bmcl.2011.08.074
56671794 65797 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
CHEMBL1834790 65797 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 516 7 2 7 3.9 COc1ccc([C@H]2CC[C@@H](N3CC(NC(=O)CNc4nn(C)c5ccc(C(F)(F)F)cc45)C3)CC2)cn1 10.1016/j.bmcl.2011.08.074
44425634 142018 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL387587 142018 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
44442599 93649 0 None 31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
CHEMBL246804 93649 0 None 31 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 585 9 5 5 3.3 Cc1cc(Br)ccc1CNC[C@H](NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1N)C(=O)NC(C)(C)C 10.1016/j.bmcl.2007.07.028
10291634 58877 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(Cl)c(Cl)c1 10.1021/jm1012903
CHEMBL1688879 58877 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.7 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1ccc(Cl)c(Cl)c1 10.1021/jm1012903
10154979 58878 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.4 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(C(F)(F)F)c1 10.1021/jm1012903
CHEMBL1688880 58878 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 352 2 2 4 3.4 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(C(F)(F)F)c1 10.1021/jm1012903
10064487 85017 4 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
CHEMBL223907 85017 4 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 318 4 2 4 3.5 Nc1ccc(CN2CCC(Nc3cccc4cnccc34)C2)cc1 10.1016/j.bmc.2006.10.028
11585168 90688 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL239143 90688 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 15 1 5 8.2 CCCC(CCCN(CC)CC)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
57402219 71008 0 None -52 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
CHEMBL1951766 71008 0 None -52 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1-induced chemotaxis after 30 mins
ChEMBL 503 6 3 4 3.8 Cc1ccc([C@]2(O)CC[C@H](N3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cc1 10.1021/ml200030q
145961260 161431 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 476 7 1 5 5.0 COC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
CHEMBL4127096 161431 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 476 7 1 5 5.0 COC1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(Cl)c3)C2=O)CC1 10.1016/j.bmc.2018.05.027
52941377 19329 0 None -7 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
CHEMBL1290637 19329 0 None -7 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 minsAntagonist activity at mouse CCR2 assessed as inhibition of MCP1 induced chemotaxis after 30 mins
ChEMBL 531 9 2 4 4.8 CCCO[C@H]1CN([C@H]2CC[C@@H](c3ccccc3)CC2)C[C@@H]1NC(=O)CNC(=O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2010.10.020
57394970 68943 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 465 7 2 3 4.0 CC(C)C1CCC(NC(C(N)=O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922800 68943 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 465 7 2 3 4.0 CC(C)C1CCC(NC(C(N)=O)C2CCN(C(=O)/C=C/c3cc(F)c(F)c(F)c3)CC2)CC1 10.1016/j.bmcl.2011.09.113
44583282 172695 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL450231 172695 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 656 9 3 7 4.2 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCOCC2)cc1 10.1016/j.bmcl.2009.05.041
53389660 171483 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
CHEMBL4463626 171483 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 300 3 1 4 2.5 O=c1c(Cc2cccc(Cl)c2)c(C2CC2)[nH]c2ncnn12 10.1021/acs.jmedchem.9b00742
53389845 172961 0 None 45 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
CHEMBL4517518 172961 0 None 45 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assayAntagonist activity at CCR2b in human THP1 cells assessed as inhibition of human MCP1 induced calcium flux by fluo-4 dye based fluorescence assay
ChEMBL 315 3 2 5 2.1 Nc1nc2[nH]c(C3CC3)c(Cc3cccc(Cl)c3)c(=O)n2n1 10.1021/acs.jmedchem.9b00742
57344303 68931 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922789 68931 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 538 7 3 3 5.0 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmcl.2011.09.113
44353447 3775 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
785 3775 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
CHEMBL337246 3775 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 433 6 2 3 3.4 O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F 10.1016/j.bmcl.2008.02.015
44425634 142018 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
CHEMBL387587 142018 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 578 6 1 2 8.0 CCC[C@]1(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@H](N2CC[C@]3(C=Cc4ccccc43)[C@@H](C)C2)C1 10.1016/j.bmcl.2008.01.023
11192346 2024 57 None -4 3 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
9032 2024 57 None -4 3 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
CHEMBL2029422 2024 57 None -4 3 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse CCR2Antagonist activity at mouse CCR2
ChEMBL 568 7 3 7 3.3 O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F 10.1021/ml200199c
44583281 188235 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL499467 188235 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 626 9 3 6 4.5 CSc1ccc(S(=O)(=O)C[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)N2CCC2)cc1 10.1016/j.bmcl.2009.05.041
49763575 65445 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
CHEMBL1829637 65445 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 474 6 3 4 3.0 N[C@]1(c2ccccc2)CC[C@H](N2CC(NC(=O)CNC(=O)c3cccc(C(F)(F)F)c3)C2)CC1 10.1016/j.bmcl.2011.06.080
24801522 161137 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
CHEMBL411726 161137 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxisAntagonist activity at human CCR2 in PBMCs assessed as inhibition of chemotaxis
ChEMBL 573 6 3 3 3.9 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@H]1CCCC[C@H]1NC(=O)c1ccc(I)cc1 10.1021/jm701488f
46884855 8303 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1092656 8303 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 548 8 2 4 3.7 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCC2CCN(C(=O)c3cccc(F)c3)CC2)C1 10.1016/j.bmcl.2010.02.072
122181235 121850 0 None 5 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
CHEMBL3589949 121850 0 None 5 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 572 7 1 3 6.7 CC1Cc2ccccc2C2(CCN(CCC(C(=O)NCc3cc(F)cc(C(F)(F)F)c3)c3ccc(F)cc3)CC2)O1 10.1016/j.bmc.2015.02.019
9923015 58876 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 318 2 2 4 3.0 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(Cl)c1 10.1021/jm1012903
CHEMBL1688878 58876 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxisAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis
ChEMBL 318 2 2 4 3.0 O=C(NC(=O)c1ccc2c(c1)OCO2)Nc1cccc(Cl)c1 10.1021/jm1012903
11582651 75203 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036754 75203 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 424 5 1 3 4.3 O=C(Nc1ccc(Cl)c(Cl)c1)N1CCN(C[C@@H]2CCCN(CC3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
145961759 161530 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 566 6 1 5 7.1 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(CC1)SCc1ccccc12 10.1016/j.bmc.2018.05.027
CHEMBL4128487 161530 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 566 6 1 5 7.1 O=C1c2ccnc(Nc3ccc(Cl)c(Cl)c3)c2CCCN1CCCN1CCC2(CC1)SCc1ccccc12 10.1016/j.bmc.2018.05.027
57656921 75213 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
CHEMBL2036764 75213 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 420 4 1 3 3.5 O=C(Nc1ccc(Br)cc1)N1CCN(C[C@@H]2CCCN(C3CC3)C2)CC1 10.1016/j.bmcl.2012.04.118
122181152 121706 0 None 25 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
CHEMBL3588870 121706 0 None 25 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 638 8 1 4 7.2 COc1ccc2c(c1)CCOC21CCN(CCC(C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccc(F)cc2)CC1 10.1016/j.bmc.2015.02.019
46241610 83570 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
CHEMBL2204252 83570 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrsAntagonist activity against CCR2 in human THP-1 cells assessed as inhibition of MCP-1 induced chemotaxis after 3 hrs
ChEMBL 548 7 3 6 3.6 CC(C)(C)Oc1ccc([C@]2(O)CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)cn1 10.1021/ml300260s
122181238 121853 0 None 194 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
CHEMBL3589952 121853 0 None 194 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 554 7 1 3 6.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)C1CC1 10.1016/j.bmc.2015.02.019
10304021 73720 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
CHEMBL2018384 73720 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 594 12 5 6 4.8 CCC[C@H](O)[C@H](CNCc1ccc(C)cc1C)NC(=O)CNC(=O)c1cc(C(F)(F)F)ccc1NC(=O)OC(C)(C)C 10.1016/j.bmcl.2012.03.007
11504634 186036 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 4.6 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
CHEMBL487070 186036 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 526 6 2 4 4.6 O=C(O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ncccc23)CC1 10.1016/j.bmcl.2008.10.061
56678508 65801 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
CHEMBL1834794 65801 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 492 6 2 7 4.0 Cn1nc(NCC(=O)NC2CN([C@H]3CC[C@@H](c4nccs4)CC3)C2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.08.074
44570718 183833 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
CHEMBL480621 183833 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMCs assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 533 9 4 5 3.2 CC(=O)Nc1ccc(CNC2CC(N(C)C)CCC2NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.12.062
44580590 193571 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
CHEMBL526859 193571 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 565 10 4 6 3.5 CCCCN1CCC(NC(=O)c2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123
46944853 65430 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
CHEMBL1829621 65430 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 490 7 2 5 3.4 COc1cc([C@H]2CC[C@H](N3CC(NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)ccn1 10.1016/j.bmcl.2011.06.080
49763574 65444 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
CHEMBL1829636 65444 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at CCR2 in human THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 477 6 2 3 4.0 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)NC1CN([C@H]2CC[C@](F)(c3ccccc3)CC2)C1 10.1016/j.bmcl.2011.06.080
54755083 65744 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
CHEMBL1834636 65744 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrsAntagonist activity at human CCR2 receptor in THP1 cells assessed as inhibition of MCP1-induced chemotaxis after 3 hrs
ChEMBL 488 6 3 6 3.1 O=C(CNc1n[nH]c2ccc(C(F)(F)F)cc12)NC1CN([C@H]2CC[C@@H](n3ccccc3=O)CC2)C1 10.1016/j.bmcl.2011.08.074
46885029 8249 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
CHEMBL1092343 8249 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.4 Cc1cccc(C(=O)N2CCN(CCN3CC[C@@H](NC(=O)CNC(=O)c4cccc(C(F)(F)F)c4)C3)CC2)c1 10.1016/j.bmcl.2010.02.072
10315045 143575 5 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
CHEMBL389926 143575 5 None - 1 Human 4.8 pIC50 = 4.8 Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
ChEMBL 337 4 1 3 4.6 Clc1ccccc1CN1CCC(Nc2cccc3cnccc23)C1 10.1016/j.bmc.2006.10.028
122181153 121840 0 None 20 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
CHEMBL3589847 121840 0 None 20 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 558 7 1 3 6.3 O=C(NCc1cc(F)cc(C(F)(F)F)c1)C(CCN1CCC2(CC1)OCCc1ccccc12)c1ccc(F)cc1 10.1016/j.bmc.2015.02.019
44416274 158554 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
CHEMBL409162 158554 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 510 6 1 2 6.4 C[C@H]1CN(CCCC(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC[C@@]12C=Cc1ccccc12 10.1016/j.bmcl.2008.01.023
10346048 78234 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL210606 78234 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
145962546 161410 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 6 3.8 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4126779 161410 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 537 8 1 6 3.8 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3ccc(Cl)c(F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
11553070 75200 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
CHEMBL2036751 75200 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 398 4 1 3 3.9 CCN1CCC[C@@H](CN2CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)C1 10.1016/j.bmcl.2012.04.118
10346048 78234 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
CHEMBL210606 78234 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR2b receptorAntagonist activity at human CCR2b receptor
ChEMBL 505 8 2 3 5.3 O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)[C@@H](NCCN1CCCCC1)c1ccc(F)cc1 10.1016/j.bmcl.2008.01.023
11563451 151918 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL396621 151918 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 608 15 1 5 8.4 CCN(CC)CCCC(CC(C)C)NC(=O)CCOc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
24801690 98041 25 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
CHEMBL273083 98041 25 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate reader assay
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1016/j.bmcl.2009.05.041
70689914 74552 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
CHEMBL2029571 74552 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopyAntagonist activity at CCR2 receptor in human PBMC assessed as inhibition of MCP1-mediated leukocyte chemotaxis after 30 mins by microscopy
ChEMBL 552 6 2 9 3.0 N#Cc1ccnc(N2CCC(C(=O)N3CC[C@H](N[C@H]4CC[C@@](O)(c5ccc(-c6ncccn6)cn5)CC4)C3)CC2)c1 10.1021/ml200199c
24801690 98041 25 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
CHEMBL273083 98041 25 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium fluxAntagonist activity at human CCR2 in PBMCs assessed as inhibition of MCP1-induced calcium flux
ChEMBL 593 9 5 5 4.5 CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 10.1021/jm701488f
44453366 158304 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
CHEMBL408908 158304 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxisAntagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
ChEMBL 451 6 5 6 1.7 Nc1cc(CN2CC[C@@H](NC(=O)CNC(=O)c3cc(C(F)(F)F)ccc3N)C2)ccc1O 10.1016/j.bmcl.2008.02.015
46885027 8421 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093469 8421 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 531 8 2 5 2.1 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3)CC2)C1 10.1016/j.bmcl.2010.02.072
53322810 58472 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683075 58472 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 499 6 1 7 2.7 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3nccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54585107 62561 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782567 62561 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assayAntagonist activity at human CCR2 assessed as inhibition of MCP1-induced chemotaxis by cell based assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ccnc(C(F)(F)F)c3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
54580188 62567 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1782573 62567 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 504 6 1 7 3.4 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3ncc(C(F)(F)F)s3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
53325639 58470 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
CHEMBL1683073 58470 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR2 by whole blood assayAntagonist activity at human CCR2 by whole blood assay
ChEMBL 498 6 1 6 3.3 CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@@](C(=O)N2CCN(c3cccc(C(F)(F)F)n3)CC2)(C(C)C)C1 10.1016/j.bmcl.2011.01.034
122181147 121835 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 464 6 1 3 4.8 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
CHEMBL3589842 121835 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assayAntagonist activity against human CCR2B expressed in Chem-1 cells assessed as inhibition of human CCL2-induced intracellular calcium flux incubated for 10 mins by Fluo-4 AM dye based intracellular calcium flux assay
ChEMBL 464 6 1 3 4.8 O=C(CCCN1CCC2(CC1)OCCc1ccccc12)NCc1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmc.2015.02.019
11670910 88622 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL235657 88622 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 524 6 2 3 4.6 NC(=O)C(C1CCN(C(=O)/C=C/c2cc(F)c(F)c(F)c2)CC1)N1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2011.09.113
145961961 161496 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.0 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(C(F)(F)F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
CHEMBL4128015 161496 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assayAntagonist activity at CCR2 (unknown origin) expressed in CHOK1 cells co-expressing Ga16 assessed as inhibition of CCL2 induced intracellular Ca2+ mobilization preincubated for 10 mins followed by CCL2 addition by fluo-4 AM dye based assay
ChEMBL 553 8 1 6 4.0 CN(C1CCN(CCCN2CCCc3c(ccnc3Nc3cccc(C(F)(F)F)c3)C2=O)CC1)S(C)(=O)=O 10.1016/j.bmc.2018.05.027
57656640 75211 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
CHEMBL2036762 75211 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysisAntagonist activity at human CCR2 receptor expressed in human THP-1 cells assessed as inhibition of MCP1-induced Ca2+ flux by FLIPR analysis
ChEMBL 390 4 1 3 3.7 Cc1ccc(NC(=O)N2CCN(C[C@@H]3CCCN(C4CC4)C3)CC2)cc1Cl 10.1016/j.bmcl.2012.04.118
44439155 91974 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
CHEMBL241497 91974 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytesAntagonist activity against human CCR2 receptor assessed as inhibition of MCP1-induced migration of human peripheral blood monocytes
ChEMBL 594 12 4 6 5.2 COC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCc1cc(-c2cc(Cl)cc(Cl)c2)nn1-c1ccc2ccccc2c1 10.1016/j.bmcl.2006.10.060
46885269 7903 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CCN(C(=O)c2ccccc2)CC1)N1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1090148 7903 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium levelAntagonist activity at human CCR2B receptor expressed in HEK293 cells assessed as inhibition of MCP1-induced increase in intracellular calcium level
ChEMBL 545 8 2 5 2.5 CC(CN1CCN(C(=O)c2ccccc2)CC1)N1CC[C@@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2010.02.072
56643545 68960 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
CHEMBL1922823 68960 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 520 7 3 3 4.9 NC(=O)C(NC1CCC(c2c[nH]c3ccccc23)CC1)C1CCN(C(=O)/C=C/c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.09.113
57398494 68958 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 527 8 3 4 4.7 CN(C)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
CHEMBL1922820 68958 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR2Antagonist activity at human CCR2
ChEMBL 527 8 3 4 4.7 CN(C)c1ccc(/C=C/C(=O)N2CCC(C(NC3CCC(c4c[nH]c5ccccc45)CC3)C(N)=O)CC2)cc1 10.1016/j.bmcl.2011.09.113
22143104 188058 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
CHEMBL497780 188058 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assayAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced calcium flux by fluorescence-imaging plate assay
ChEMBL 483 7 5 5 2.3 Nc1ccc(C(F)(F)F)cc1C(=O)NCC(=O)NC1CNCCC1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.123
22143294 193426 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxisAntagonist activity at CCR2 in human PBMC assessed as MCP1-induced chemotaxis
ChEMBL 551 11 4 6 3.9 CCCCN1CCC(NCc2ccc(SC)cc2)C(NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2N)C1 10.1016/j.bmcl.2008.07.123<